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Ref Type Journal Article
PMID (40526877)
Authors Ziegler M, Khoury N, Hommerich LM, Adler H, Loges S
Title Functional Characterization of Variants of Unknown Significance of Fibroblast Growth Factor Receptors 1-4 and Comparison With AI Model-Based Prediction.
URL
Abstract Text Fibroblast growth factor receptors (FGFRs; FGFR1, FGFR2, FGFR3, FGFR4) are frequently mutated oncogenes in solid cancers. The oncogenic potential of FGFR rearrangements and few hotspot point mutations is well established, but the majority of variants resulting from point mutations especially outside of the tyrosine kinase domain are currently considered variants of unknown significance (VUS).Recurrent nonkinase domain FGFR VUS variants were collected from the Catalog of Somatic Mutations in Cancer and their oncogenic potential was assessed in vitro by different functional assays. We compiled published clinical and preclinical data on FGFR variants and compared the data with results from our functional assays and pathogenicity predictions of state-of-the-art artificial intelligence (AI) models.We identified 12 novel FGFR extracellular small variants with potential driver function. Comparison of clinical and preclinical data on FGFR variants with pathogenicity predictions of state-of-the-art AI models showed limited usefulness of the AI predictions. Sensitivity profiles of activating FGFR variants to targeted inhibitors were recorded and showed good targetability of FGFR nonkinase domain variants.The collected results extend the spectrum of suitable FGFR variants for potential treatment with FGFR inhibitors in the context of clinical trials and beyond. Current AI models for variant pathogenicity prediction require further refinement for use in oncogenic decision making.

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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
Drug Name Trade Name Synonyms Drug Classes Drug Description
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
FGFR1 C381R missense gain of function FGFR1 C381R lies within the transmembrane domain of the Fgfr1 protein (UniProt.org). C381R is associated with increased phospho-Erk1/2 staining in a patient tumor sample (PMID: 30385747), increased proliferation and anchorage-independent colony formation in culture (PMID: 40526877), and the corresponding variant in an alternate isoform (C379R) demonstrates constitutive Fgfr1 activity in a luciferase assay and increased Erk1/2 phosphorylation in cell culture (PMID: 26272615).
FGFR1 D218N missense loss of function - predicted FGFR1 D218N lies within Ig-like C2-type domain 2 of the Fgfr1 protein (UniProt.org). D218N results in increased serum dependency for growth in culture (PMID: 40526877), and therefore, is predicted to lead to a loss of Fgfr1 protein function.
FGFR1 P222L missense loss of function - predicted FGFR1 P222L lies within Ig-like C2-type domain 2 of the Fgfr1 protein (UniProt.org). P222L results in increased serum dependency for growth in culture (PMID: 40526877), and therefore, is predicted to lead to a loss of Fgfr1 protein function.
FGFR1 P283L missense unknown FGFR1 P283L lies within Ig-like C2-type domain 3 of the Fgfr1 protein (UniProt.org). P283L does not significantly alter serum dependency for growth in cell culture (PMID: 40526877), but has not been fully biochemically characterized and therefore, its effect on Fgfr1 protein function is unknown.
FGFR1 P285S missense loss of function - predicted FGFR1 P285S lies within Ig-like C2-type domain 3 of the Fgfr1 protein (UniProt.org). P285S results in increased serum dependency for growth in culture (PMID: 40526877), and therefore, is predicted to lead to a loss of Fgfr1 protein function.
FGFR1 R189C missense gain of function - predicted FGFR1 R189C lies within Ig-like C2-type domain 2 of the Fgfr1 protein (UniProt.org). R189C results in transformation activity similar to wild-type Fgfr1 but an increased growth advantage in a competition assay (PMID: 34272467), increased proliferation, and anchorage-independent colony formation in cultured cells (PMID: 40526877), and therefore, is predicted to lead to a gain of Fgfr1 protein function.
FGFR1 R250W missense unknown FGFR1 R250W lies within the D2-D3 linker region of the Fgfr1 protein (PMID: 23276709). R250W results in similar cell proliferation and viability levels to wild-type Fgfr1 in two different cell lines in culture in one study (PMID: 29533785), increased proliferation and anchorage-independent colony formation in another study (PMID: 40526877), decreased proliferation relative to wild-type Fgfr1 in a competition assay, and transformation activity similar to wild-type Fgfr1 in another study (PMID: 34272467), and therefore, its effect on Fgfr1 protein function is unknown.
FGFR1 R470C missense unknown FGFR1 R470C lies within the cytoplasmic domain of the Fgfr1 protein (UniProt.org). R470C does not significantly alter serum dependency for growth in cell culture (PMID: 40526877), but has not been fully biochemically characterized and therefore, its effect on Fgfr1 protein function is unknown.
FGFR1 R54C missense gain of function - predicted FGFR1 R54C lies within Ig-like C2-type domain 1 of the Fgfr1 protein (UniProt.org). R54C results in anchorage-independent colony formation similar to wild-type Fgfr1 but increased proliferation in culture (PMID: 40526877), and therefore, is predicted to lead to a gain of Fgfr1 protein function.
FGFR1 S393L missense loss of function - predicted FGFR1 S393L lies within the transmembrane domain of the Fgfr1 protein (UniProt.org). S393L results in increased serum dependency for growth in culture (PMID: 40526877), and therefore, is predicted to lead to a loss of Fgfr1 protein function.
FGFR1 S42C missense gain of function - predicted FGFR1 S42C lies within Ig-like C2-type domain 1 of the Fgfr1 protein (UniProt.org). S42C results in increased proliferation and anchorage-independent colony formation in culture (PMID: 40526877), and therefore, is predicted to lead to a gain of Fgfr1 protein function.
FGFR1 V561M missense gain of function FGFR1 V561M lies within the protein kinase domain of the Fgfr1 protein (UniProt.org). V561M results in increased Fgfr1 autophosphorylation (PMID: 25686244), increased Stat3 phosphorylation and STAT3-dependent gene expression, elevated expression of mesenchymal genes, and increased migration (PMID: 30257990), cell proliferation, and anchorage-independent growth in culture (PMID: 30257990, PMID: 40526877), and has been shown to be associated with resistance to tyrosine kinase inhibitors (PMID: 25686244, PMID: 40526877, PMID: 28646488), Y
FGFR2 A53V missense unknown FGFR2 A53V lies within Ig-like C2-type domain 1 of the Fgfr2 protein (UniProt.org). A53V does not significantly alter serum dependency for growth in cell culture (PMID: 40526877), but has not been fully biochemically characterized and therefore, its effect on Fgfr2 protein function is unknown.
FGFR2 D75N missense gain of function - predicted FGFR2 D75N lies within Ig-like C2-type domain 1 of the Fgfr2 protein (UniProt.org). D75N results in decreased serum dependency for growth in culture (PMID: 40526877), and therefore, is predicted to lead to a gain of Fgfr2 protein function.
FGFR2 H254Y missense gain of function FGFR2 H254Y lies within the extracellular domain of the Fgfr2 protein (UniProt.org). H254Y leads to a gain of Fgfr2 protein function as indicated by decreased serum dependency for growth and anchorage-independent colony formation in culture (PMID: 40526877).
FGFR2 R210* nonsense loss of function - predicted FGFR2 R210* results in a premature truncation of the Fgfr2 protein at amino acid 210 of 821 (UniProt.org). R210* results in increased serum dependency for growth in culture (PMID: 40526877), and therefore, is predicted to lead to a loss of Fgfr2 protein function.
FGFR2 R425W missense loss of function - predicted FGFR2 R425W lies within the cytoplasmic domain of the Fgfr2 protein (UniProt.org). R425W results in increased serum dependency for growth in culture (PMID: 40526877), and therefore, is predicted to lead to a loss of Fgfr2 protein function.
FGFR2 R450H missense gain of function FGFR2 R450H lies within the cytoplasmic domain of the Fgfr2 protein (UniProt.org). R450H leads to a gain of Fgfr2 protein function as indicated by decreased serum dependency for growth and anchorage-independent colony formation in culture (PMID: 40526877).
FGFR2 R478K missense unknown FGFR2 R478K lies within the cytoplasmic domain of the Fgfr2 protein (UniProt.org). R478K does not significantly alter serum dependency for growth in cell culture (PMID: 40526877), but has not been fully biochemically characterized and therefore, its effect on Fgfr2 protein function is unknown.
FGFR2 S252W missense gain of function FGFR2 S252W lies within the extracellular domain of the Fgfr2 protein (UniProt.org). S252W results in a growth advantage relative to wild-type Fgfr2 in a competition assay and transformation activity similar to overexpressed Fgfr2 in cultured cells (PMID: 34272467), and results in decreased serum dependency for growth (PMID: 40526877), loss of ligand specificity, increased Fgfr2 phosphorylation, increased FGF7-stimulated shedding of HB-EGF, and is transforming in cell culture (PMID: 11121055, PMID: 18552176, PMID: 37759450).
FGFR2 S351C missense gain of function FGFR2 S351C lies within Ig-like C2-type domain 3 of the Fgfr2 protein (UniProt.org). S351C leads to a gain of Fgfr2 protein function as indicated by decreased serum dependency for growth and anchorage-independent colony formation in culture (PMID: 40526877).
FGFR2 T320M missense gain of function - predicted FGFR2 T320M lies within Ig-like C2-type domain 3 of the Fgfr2 protein (UniProt.org). T320M results in colony formation similar to wild-type Fgfr2 but decreased serum dependency for growth in culture (PMID: 40526877), and therefore, is predicted to lead to a gain of Fgfr2 protein function.
FGFR2 V12M missense loss of function - predicted FGFR2 V12M does not lie within any known functional domains of the Fgfr2 protein (UniProt.org). V12M results in increased serum dependency for growth in culture (PMID: 40526877), and therefore, is predicted to lead to a loss of Fgfr2 protein function.
FGFR2 W290R missense gain of function FGFR2 W290R lies within Ig-like C2-type domain 3 of the Fgfr2 protein (UniProt.org). W290R leads to a gain of Fgfr2 protein function as indicated by decreased serum dependency for growth and anchorage-independent colony formation in culture (PMID: 40526877).
FGFR3 A179T missense unknown FGFR3 A179T lies within Ig-like C2-type domain 2 of the Fgfr3 protein (UniProt.org). A179T does not significantly alter serum dependency for growth in cell culture (PMID: 40526877), but has not been fully biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown.
FGFR3 A312V missense unknown FGFR3 A312V lies within Ig-like C2-type domain 3 of the Fgfr3 protein (UniProt.org). A312V does not significantly alter serum dependency for growth in cell culture (PMID: 40526877), but has not been fully biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown.
FGFR3 A441T missense unknown FGFR3 A441T lies within the cytoplasmic domain of the Fgfr3 protein (UniProt.org). A441T does not significantly alter serum dependency for growth in cell culture (PMID: 40526877), but has not been fully biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown.
FGFR3 F386L missense unknown FGFR3 F386L lies within the transmembrane domain of the Fgfr3 protein (UniProt.org). F386L has been reported as a polymorphism (PMID: 19377444, PMID: 16877735) and does not significantly alter serum dependency for growth in cell culture (PMID: 40526877), but has not been fully biochemically characterized and therefore, its effect on Fgfr4 protein function is unknown.
FGFR3 G197S missense unknown FGFR3 G197S lies within Ig-like C2-type domain 2 of the Fgfr3 protein (UniProt.org). G197S does not significantly alter serum dependency for growth in cell culture (PMID: 40526877), but has not been fully biochemically characterized and therefore, its effect on Fgfr4 protein function is unknown.
FGFR3 G299S missense unknown FGFR3 G299S lies within Ig-like C2-type domain 3 of the Fgfr3 protein (UniProt.org). G299S does not significantly alter serum dependency for growth in cell culture (PMID: 40526877), but has not been fully biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown.
FGFR3 P250S missense unknown FGFR3 P250S lies within the extracellular domain of the Fgfr3 protein (UniProt.org). P250S does not significantly alter serum dependency for growth in cell culture (PMID: 40526877), but has not been fully biochemically characterized and therefore, its effect on Fgfr4 protein function is unknown.
FGFR3 P418S missense unknown FGFR3 P418S lies within the cytoplasmic domain of the Fgfr3 protein (UniProt.org). P418S does not significantly alter serum dependency for growth in cell culture (PMID: 40526877), but has not been fully biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown.
FGFR3 P449S missense unknown FGFR3 P449S lies within the cytoplasmic domain of the Fgfr3 protein (UniProt.org). P449S does not significantly alter serum dependency for growth in cell culture (PMID: 40526877), but has not been fully biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown.
FGFR3 R175C missense unknown FGFR3 R175C lies within Ig-like C2-type domain 2 of the Fgfr3 protein (UniProt.org). R175C does not significantly alter serum dependency for growth in cell culture (PMID: 40526877), but has not been fully biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown.
FGFR3 R252Q missense unknown FGFR3 R252Q lies within the extracellular domain of the Fgfr3 protein (UniProt.org). R252Q does not significantly alter serum dependency for growth in cell culture (PMID: 40526877), but has not been fully biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown.
FGFR3 R416C missense unknown FGFR3 R416C lies within the cytoplasmic domain of the Fgfr3 protein (UniProt.org). R416C does not significantly alter serum dependency for growth in cell culture (PMID: 40526877), but has not been fully biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown.
FGFR3 S130F missense unknown FGFR3 S130F lies within the extracellular domain of the Fgfr3 protein (UniProt.org). S130F does not significantly alter serum dependency for growth in cell culture (PMID: 40526877), but has not been fully biochemically characterized and therefore, its effect on Fgfr3 protein function is unknown.
FGFR3 S131L missense unknown FGFR3 S131L lies within the extracellular domain of the Fgfr3 protein (UniProt.org). The functional effect of S131L is conflicting, as it results in decreased proliferation and cell viability compared to wild-type Fgfr3 in one study (PMID: 29533785), however, demonstrates increased cell proliferation under some cell culture conditions (PMID: 27053219) and does not significantly alter serum dependency for growth in culture (PMID: 40526877), and therefore, its effect on Fgfr3 protein function is unknown.
FGFR3 S424F missense gain of function - predicted FGFR3 S424F lies within the cytoplasmic domain of the Fgfr3 protein (UniProt.org). S424F results in decreased serum dependency for growth in culture (PMID: 40526877), and therefore, is predicted to lead to a gain of Fgfr3 protein function.
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
FGFR2 S351C Advanced Solid Tumor sensitive Pemigatinib Preclinical - Cell culture Actionable In a preclinical study, Pemazyre (pemigatinib) inhibited viability of cells expressing FGFR2 S351C in culture (PMID: 40526877). 40526877
FGFR1 C381R Advanced Solid Tumor sensitive Pemigatinib Preclinical - Cell culture Actionable In a preclinical study, Pemazyre (pemigatinib) inhibited viability of cells expressing FGFR1 C381R in culture (PMID: 40526877). 40526877
FGFR2 S267P Advanced Solid Tumor sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, Fexagratinib (AZD4547) inhibited viability of cells expressing FGFR2 S267P in culture (PMID: 40526877). 40526877
FGFR1 S42C Advanced Solid Tumor sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Lytgobi (futibatinib) inhibited viability of cells expressing FGFR1 S42C in culture (PMID: 40526877). 40526877
FGFR1 C178S Advanced Solid Tumor sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, Fexagratinib (AZD4547) inhibited viability of cells expressing FGFR1 C178S in culture (PMID: 40526877). 40526877
FGFR1 C178S Advanced Solid Tumor sensitive Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited viability of cells expressing FGFR1 C178S in culture (PMID: 40526877). 40526877
FGFR3 K508M Advanced Solid Tumor resistant Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR3 K508M were resistant to Balversa (erdafitinib) in culture (PMID: 40526877). 40526877
FGFR2 S351C Advanced Solid Tumor sensitive Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited viability of cells expressing FGFR2 S351C in culture (PMID: 40526877). 40526877
FGFR1 K656E Advanced Solid Tumor sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, Fexagratinib (AZD4547) inhibited viability of cells expressing FGFR1 K656E in culture (PMID: 40526877). 40526877
FGFR2 E116K Advanced Solid Tumor sensitive Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited viability of cells expressing FGFR2 E116K in culture (PMID: 40526877). 40526877
FGFR2 G338R Advanced Solid Tumor sensitive Pemigatinib Preclinical - Cell culture Actionable In a preclinical study, Pemazyre (pemigatinib) inhibited viability of cells expressing FGFR2 G338R in culture (PMID: 40526877). 40526877
FGFR1 C178S Advanced Solid Tumor sensitive Pemigatinib Preclinical - Cell culture Actionable In a preclinical study, Pemazyre (pemigatinib) inhibited viability of cells expressing FGFR1 C178S in culture (PMID: 40526877). 40526877
FGFR1 S42C Advanced Solid Tumor sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, Fexagratinib (AZD4547) inhibited viability of cells expressing FGFR1 S42C in culture (PMID: 40526877). 40526877
FGFR2 S267P Advanced Solid Tumor sensitive Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited viability of cells expressing FGFR2 S267P in culture (PMID: 40526877). 40526877
FGFR2 E116K Advanced Solid Tumor sensitive Pemigatinib Preclinical - Cell culture Actionable In a preclinical study, Pemazyre (pemigatinib) inhibited viability of cells expressing FGFR2 E116K in culture (PMID: 40526877). 40526877
FGFR1 C381R Advanced Solid Tumor sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, Fexagratinib (AZD4547) inhibited viability of cells expressing FGFR1 C381R in culture (PMID: 40526877). 40526877
FGFR1 A121D Advanced Solid Tumor sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Lytgobi (futibatinib) inhibited viability of cells expressing FGFR1 A121D in culture (PMID: 40526877). 40526877
FGFR1 S42C Advanced Solid Tumor sensitive Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited colony formation in cells expressing FGFR1 S42C in culture (PMID: 40526877). 40526877
FGFR1 R189C Advanced Solid Tumor sensitive Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited viability of cells expressing FGFR1 R189C in culture (PMID: 40526877). 40526877
FGFR1 C381R Advanced Solid Tumor sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Lytgobi (futibatinib) inhibited viability of cells expressing FGFR1 C381R in culture (PMID: 40526877). 40526877
FGFR2 R450H Advanced Solid Tumor sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, Fexagratinib (AZD4547) inhibited viability of cells expressing FGFR2 R450H in culture (PMID: 40526877). 40526877
FGFR3 S424F Advanced Solid Tumor sensitive Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited viability of cells expressing FGFR3 S424F in culture (PMID: 40526877). 40526877
FGFR2 S351C Advanced Solid Tumor sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Lytgobi (futibatinib) inhibited viability of cells expressing FGFR2 S351C in culture (PMID: 40526877). 40526877
FGFR3 R248C Advanced Solid Tumor sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Lytgobi (futibatinib) inhibited viability of cells expressing FGFR3 R248C in culture (PMID: 40526877). 40526877
FGFR1 R250W Advanced Solid Tumor sensitive Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited viability of cells expressing FGFR1 R250W in culture (PMID: 40526877). 40526877
FGFR3 K508M Advanced Solid Tumor resistant Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR3 K508M were resistant to Fexagratinib (AZD4547) in culture (PMID: 40526877). 40526877
FGFR2 C382R Advanced Solid Tumor sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Lytgobi (futibatinib) inhibited viability of cells expressing FGFR2 C382R in culture (PMID: 40526877). 40526877
FGFR2 E219K Advanced Solid Tumor sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Lytgobi (futibatinib) inhibited viability of cells expressing FGFR2 E219K in culture (PMID: 40526877). 40526877
FGFR3 V50I Advanced Solid Tumor resistant Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR3 V50I were resistant to Balversa (erdafitinib) in culture (PMID: 40526877). 40526877
FGFR1 R189C Advanced Solid Tumor sensitive Pemigatinib Preclinical - Cell culture Actionable In a preclinical study, Pemazyre (pemigatinib) inhibited viability of cells expressing FGFR1 R189C in culture (PMID: 40526877). 40526877
FGFR2 P253R Advanced Solid Tumor sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, Fexagratinib (AZD4547) inhibited viability of cells expressing FGFR2 P253R in culture (PMID: 40526877). 40526877
FGFR2 W290R Advanced Solid Tumor sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Lytgobi (futibatinib) inhibited viability of cells expressing FGFR2 W290R in culture (PMID: 40526877). 40526877
FGFR1 C178S Advanced Solid Tumor sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Lytgobi (futibatinib) inhibited viability of cells expressing FGFR1 C178S in culture (PMID: 40526877). 40526877
FGFR1 K656E Advanced Solid Tumor conflicting Pemigatinib Preclinical - Cell culture Actionable In a preclinical study, Pemazyre (pemigatinib) inhibited viability of cells expressing FGFR1 K656E in culture (PMID: 40526877). 40526877
FGFR2 R450H Advanced Solid Tumor sensitive Pemigatinib Preclinical - Cell culture Actionable In a preclinical study, Pemazyre (pemigatinib) inhibited viability of cells expressing FGFR2 R450H in culture (PMID: 40526877). 40526877
FGFR1 V561M Advanced Solid Tumor resistant Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 V561M were resistant to Fexagratinib (AZD4547) in culture (PMID: 40526877). 40526877
FGFR2 S267P Advanced Solid Tumor sensitive Pemigatinib Preclinical - Cell culture Actionable In a preclinical study, Pemazyre (pemigatinib) inhibited viability of cells expressing FGFR2 S267P in culture (PMID: 40526877). 40526877
FGFR2 P253R Advanced Solid Tumor sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Lytgobi (futibatinib) inhibited viability of cells expressing FGFR2 P253R in culture (PMID: 40526877). 40526877
FGFR2 W290R Advanced Solid Tumor sensitive Pemigatinib Preclinical - Cell culture Actionable In a preclinical study, Pemazyre (pemigatinib) inhibited viability of cells expressing FGFR2 W290R in culture (PMID: 40526877). 40526877
FGFR1 R54C Advanced Solid Tumor sensitive Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited viability of cells expressing FGFR1 R54C in culture (PMID: 40526877). 40526877
FGFR2 E116K Advanced Solid Tumor sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Lytgobi (futibatinib) inhibited viability of cells expressing FGFR2 E116K in culture (PMID: 40526877). 40526877
FGFR1 V561M Advanced Solid Tumor resistant Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 V561M were resistant to Balversa (erdafitinib) in culture (PMID: 40526877). 40526877
FGFR1 R54C Advanced Solid Tumor sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Lytgobi (futibatinib) inhibited viability of cells expressing FGFR1 R54C in culture (PMID: 40526877). 40526877
FGFR2 S252W Advanced Solid Tumor sensitive Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited viability of cells expressing FGFR2 S252W in culture (PMID: 40526877). 40526877
FGFR2 P253R Advanced Solid Tumor sensitive Pemigatinib Preclinical - Cell culture Actionable In a preclinical study, Pemazyre (pemigatinib) inhibited viability of cells expressing FGFR2 P253R in culture (PMID: 40526877). 40526877
FGFR1 K656E Advanced Solid Tumor sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Lytgobi (futibatinib) inhibited viability of cells expressing FGFR1 K656E in culture (PMID: 40526877). 40526877
FGFR1 V561M Advanced Solid Tumor resistant Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 V561M were resistant to Lytgobi (futibatinib) in culture (PMID: 40526877). 40526877
FGFR1 A121D Advanced Solid Tumor sensitive Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited colony formation in cells expressing FGFR1 A121D in culture (PMID: 40526877). 40526877
FGFR2 Y340C Advanced Solid Tumor sensitive Pemigatinib Preclinical - Cell culture Actionable In a preclinical study, Pemazyre (pemigatinib) inhibited viability of cells expressing FGFR2 Y340C in culture (PMID: 40526877). 40526877
FGFR2 G338R Advanced Solid Tumor sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Lytgobi (futibatinib) inhibited viability of cells expressing FGFR2 G338R in culture (PMID: 40526877). 40526877
FGFR3 S249C Advanced Solid Tumor sensitive Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited viability of cells expressing FGFR3 S249C in culture (PMID: 40526877). 40526877
FGFR1 K656E Advanced Solid Tumor conflicting Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited viability of cells expressing FGFR1 K656E in culture (PMID: 40526877). 40526877
FGFR1 R250W Advanced Solid Tumor sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Lytgobi (futibatinib) inhibited viability of cells expressing FGFR1 R250W in culture (PMID: 40526877). 40526877
FGFR1 A121D Advanced Solid Tumor sensitive Pemigatinib Preclinical - Cell culture Actionable In a preclinical study, Pemazyre (pemigatinib) inhibited viability of cells expressing FGFR1 A121D in culture (PMID: 40526877). 40526877
FGFR2 E219K Advanced Solid Tumor sensitive Pemigatinib Preclinical - Cell culture Actionable In a preclinical study, Pemazyre (pemigatinib) inhibited viability of cells expressing FGFR2 E219K in culture (PMID: 40526877). 40526877
FGFR2 H254Y Advanced Solid Tumor sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, Fexagratinib (AZD4547) inhibited viability of cells expressing FGFR2 H254Y in culture (PMID: 40526877). 40526877
FGFR2 Y375C Advanced Solid Tumor sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Lytgobi (futibatinib) inhibited viability of cells expressing FGFR2 Y375C in culture (PMID: 40526877). 40526877
FGFR1 C381R Advanced Solid Tumor sensitive Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited colony formation and viability in cells expressing FGFR1 C381R in culture (PMID: 40526877). 40526877
FGFR2 W290R Advanced Solid Tumor sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, Fexagratinib (AZD4547) inhibited viability of cells expressing FGFR2 W290R in culture (PMID: 40526877). 40526877
FGFR1 V561M Advanced Solid Tumor resistant Pemigatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 V561M were resistant to Pemazyre (pemigatinib) in culture (PMID: 40526877). 40526877
FGFR2 T320M Advanced Solid Tumor sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Lytgobi (futibatinib) inhibited viability of cells expressing FGFR2 T320M in culture (PMID: 40526877). 40526877
FGFR1 R250W Advanced Solid Tumor sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, Fexagratinib (AZD4547) inhibited viability of cells expressing FGFR1 R250W in culture (PMID: 40526877). 40526877
FGFR2 W290R Advanced Solid Tumor sensitive Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited viability of cells expressing FGFR2 W290R in culture (PMID: 40526877). 40526877
FGFR2 R450H Advanced Solid Tumor sensitive Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited viability of cells expressing FGFR2 R450H in culture (PMID: 40526877). 40526877
FGFR2 C382R Advanced Solid Tumor sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, Fexagratinib (AZD4547) inhibited viability of cells expressing FGFR2 C382R in culture (PMID: 40526877). 40526877
FGFR2 S267P Advanced Solid Tumor sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Lytgobi (futibatinib) inhibited viability of cells expressing FGFR2 S267P in culture (PMID: 40526877). 40526877
FGFR3 S424F Advanced Solid Tumor sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Lytgobi (futibatinib) inhibited viability of cells expressing FGFR3 S424F in culture (PMID: 40526877). 40526877
FGFR2 H254Y Advanced Solid Tumor sensitive Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited viability of cells expressing FGFR2 H254Y in culture (PMID: 40526877). 40526877
FGFR2 C382R Advanced Solid Tumor sensitive Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited viability of cells expressing FGFR2 C382R in culture (PMID: 40526877). 40526877
FGFR1 S42C Advanced Solid Tumor sensitive Pemigatinib Preclinical - Cell culture Actionable In a preclinical study, Pemazyre (pemigatinib) inhibited viability of cells expressing FGFR1 S42C in culture (PMID: 40526877). 40526877
FGFR3 V50I Advanced Solid Tumor resistant Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR3 V50I were resistant to Fexagratinib (AZD4547) in culture (PMID: 40526877). 40526877
FGFR3 S424F Advanced Solid Tumor sensitive Pemigatinib Preclinical - Cell culture Actionable In a preclinical study, Pemazyre (pemigatinib) inhibited viability of cells expressing FGFR3 S424F in culture (PMID: 40526877). 40526877
FGFR1 R189C Advanced Solid Tumor sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, Fexagratinib (AZD4547) inhibited viability of cells expressing FGFR1 R189C in culture (PMID: 40526877). 40526877
FGFR2 G338R Advanced Solid Tumor sensitive Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited viability of cells expressing FGFR2 G338R in culture (PMID: 40526877). 40526877
FGFR2 T320M Advanced Solid Tumor sensitive Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited viability of cells expressing FGFR2 T320M in culture (PMID: 40526877). 40526877
FGFR2 Y340C Advanced Solid Tumor sensitive Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited viability of cells expressing FGFR2 Y340C in culture (PMID: 40526877). 40526877
FGFR2 R450H Advanced Solid Tumor sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Lytgobi (futibatinib) inhibited viability of cells expressing FGFR2 R450H in culture (PMID: 40526877). 40526877
FGFR2 S252W Advanced Solid Tumor sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, Fexagratinib (AZD4547) inhibited viability of cells expressing FGFR2 S252W in culture (PMID: 40526877). 40526877
FGFR2 H254Y Advanced Solid Tumor sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Lytgobi (futibatinib) inhibited viability of cells expressing FGFR2 H254Y in culture (PMID: 40526877). 40526877
FGFR2 P253R Advanced Solid Tumor sensitive Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited viability of cells expressing FGFR2 P253R in culture (PMID: 40526877). 40526877
FGFR3 R248C Advanced Solid Tumor sensitive Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited viability of cells expressing FGFR3 R248C in culture (PMID: 40526877). 40526877
FGFR2 C382R Advanced Solid Tumor sensitive Pemigatinib Preclinical - Cell culture Actionable In a preclinical study, Pemazyre (pemigatinib) inhibited viability of cells expressing FGFR2 C382R in culture (PMID: 40526877). 40526877
FGFR2 W290C Advanced Solid Tumor sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Lytgobi (futibatinib) inhibited viability of cells expressing FGFR2 W290C in culture (PMID: 40526877). 40526877
FGFR2 S252W Advanced Solid Tumor sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Lytgobi (futibatinib) inhibited viability of cells expressing FGFR2 S252W in culture (PMID: 40526877). 40526877
FGFR2 S351C Advanced Solid Tumor sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, Fexagratinib (AZD4547) inhibited viability of cells expressing FGFR2 S351C in culture (PMID: 40526877). 40526877
FGFR1 R54C Advanced Solid Tumor sensitive Pemigatinib Preclinical - Cell culture Actionable In a preclinical study, Pemazyre (pemigatinib) inhibited viability of cells expressing FGFR1 R54C in culture (PMID: 40526877). 40526877
FGFR2 E219K Advanced Solid Tumor sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, Fexagratinib (AZD4547) inhibited viability of cells expressing FGFR2 E219K in culture (PMID: 40526877). 40526877
FGFR1 A121D Advanced Solid Tumor sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, Fexagratinib (AZD4547) inhibited viability of cells expressing FGFR1 A121D in culture (PMID: 40526877). 40526877
FGFR2 N549K Advanced Solid Tumor sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Lytgobi (futibatinib) inhibited viability of cells expressing FGFR2 N549K in culture (PMID: 40526877). 40526877
FGFR2 T320M Advanced Solid Tumor sensitive Pemigatinib Preclinical - Cell culture Actionable In a preclinical study, Pemazyre (pemigatinib) inhibited viability of cells expressing FGFR2 T320M in culture (PMID: 40526877). 40526877
FGFR2 G338R Advanced Solid Tumor sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, Fexagratinib (AZD4547) inhibited viability of cells expressing FGFR2 G338R in culture (PMID: 40526877). 40526877
FGFR2 W290C Advanced Solid Tumor sensitive Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited viability of cells expressing FGFR2 W290C in culture (PMID: 40526877). 40526877
FGFR2 E219K Advanced Solid Tumor sensitive Erdafitinib Preclinical - Cell culture Actionable In a preclinical study, Balversa (erdafitinib) inhibited viability of cells expressing FGFR2 E219K in culture (PMID: 40526877). 40526877
FGFR1 R54C Advanced Solid Tumor sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, Fexagratinib (AZD4547) inhibited viability of cells expressing FGFR1 R54C in culture (PMID: 40526877). 40526877
FGFR2 E116K Advanced Solid Tumor sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, Fexagratinib (AZD4547) inhibited viability of cells expressing FGFR2 E116K in culture (PMID: 40526877). 40526877
FGFR2 H254Y Advanced Solid Tumor sensitive Pemigatinib Preclinical - Cell culture Actionable In a preclinical study, Pemazyre (pemigatinib) inhibited viability of cells expressing FGFR2 H254Y in culture (PMID: 40526877). 40526877
FGFR2 S252W Advanced Solid Tumor sensitive Pemigatinib Preclinical - Cell culture Actionable In a preclinical study, Pemazyre (pemigatinib) inhibited viability of cells expressing FGFR2 S252W in culture (PMID: 40526877). 40526877
FGFR1 R250W Advanced Solid Tumor sensitive Pemigatinib Preclinical - Cell culture Actionable In a preclinical study, Pemazyre (pemigatinib) inhibited viability of cells expressing FGFR1 R250W in culture (PMID: 40526877). 40526877
FGFR1 R189C Advanced Solid Tumor sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Lytgobi (futibatinib) inhibited viability of cells expressing FGFR1 R189C in culture (PMID: 40526877). 40526877
FGFR2 T320M Advanced Solid Tumor sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, Fexagratinib (AZD4547) inhibited viability of cells expressing FGFR2 T320M in culture (PMID: 40526877). 40526877