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Gene | KIT |
Variant | N822K |
Impact List | missense |
Protein Effect | gain of function |
Gene Variant Descriptions | KIT N822K lies within the activation loop in the protein kinase domain of the Kit protein (PMID: 24205792). N822K results in constitutive activation of Kit, increased Erk1/2 and Stat3 phosphorylation, is transforming in culture (PMID: 24205792, PMID: 31484543), leads to mislocalization of Kit to endolysosomes (PMID: 31484543), and has been identified as a secondary mutation associated with imatinib resistance (PMID: 18488160). |
Associated Drug Resistance | Y |
Category Variants Paths |
KIT mutant KIT act mut KIT N822K KIT mutant KIT exon17 KIT N822K |
Transcript | NM_000222.3 |
gDNA | chr4:g.54733174T>G |
cDNA | c.2466T>G |
Protein | p.N822K |
Source Database | RefSeq |
Genome Build | GRCh38/hg38 |
Transcript | gDNA | cDNA | Protein | Source Database | Genome Build |
---|---|---|---|---|---|
XM_005265741 | chr4:g.54733174T>G | c.2466T>G | p.N822K | RefSeq | GRCh38/hg38 |
NM_001385290.1 | chr4:g.54733174T>G | c.2466T>G | p.N822K | RefSeq | GRCh38/hg38 |
NM_000222.3 | chr4:g.54733174T>G | c.2466T>G | p.N822K | RefSeq | GRCh38/hg38 |
XM_005265741.1 | chr4:g.54733174T>G | c.2466T>G | p.N822K | RefSeq | GRCh38/hg38 |
NM_000222 | chr4:g.54733174T>G | c.2466T>G | p.N822K | RefSeq | GRCh38/hg38 |
NM_000222.2 | chr4:g.54733174T>G | c.2466T>G | p.N822K | RefSeq | GRCh38/hg38 |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
KIT N822K | hematologic cancer | sensitive | Crenolanib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT N822K were sensitive to treatment with Crenolanib in culture, demonstrating reduced cell survival (PMID: 31182436). | 31182436 |
KIT N822K | hematologic cancer | sensitive | Dasatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT N822K were sensitive to treatment with Sprycel (dasatinib) in culture, demonstrating reduced cell survival (PMID: 31182436). | 31182436 |
KIT N822K | acute myeloid leukemia | decreased response | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, acute myeloid leukemia cells harboring KIT N822K demonstrated reduced response to growth inhibition by Gleevec (imatinib) compared to GIST cells harboring KIT exon 11 deletion in culture (PMID: 31085175). | 31085175 |
KIT N822K | gastrointestinal stromal tumor | predicted - resistant | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, KIT N822K was identified in the tumor of a gastrointestinal stromal tumor patient who was resistant to Gleevec (imatinib) treatment (PMID: 26316776). | 26316776 |
KIT N822K | Advanced Solid Tumor | resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT N822K were resistant to treatment with Gleevec (imatinib) in culture (PMID: 24205792). | 24205792 |
KIT N822K | acute myeloid leukemia | sensitive | Midostaurin | Preclinical - Cell culture | Actionable | In a preclinical study, Rydapt (midostaurin) inhibited proliferation of acute myeloid leukemia cells harboring KIT N822K in culture (PMID: 31085175). | 31085175 |
KIT N822K | leukemia | sensitive | Ponatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Iclusig (ponatinib) inhibited Kit signaling and viability in leukemia cells harboring KIT N822K in culture (PMID: 21482694). | 21482694 |
KIT N822K | acute myeloid leukemia | sensitive | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Stivarga (regorafenib) inhibited proliferation of acute myeloid leukemia cells harboring KIT N822K in culture (PMID: 31085175). | 31085175 |
KIT N822K | acute myeloid leukemia | predicted - sensitive | Sunitinib | Preclinical - Cell culture | Actionable | In a preclinical study, an acute myeloid leukemia cell line harboring KIT N822K demonstrated increased sensitivity to Sutent (sunitinib) compared to cells with wild-type KIT, resulting in increased inhibition of colony formation, and induction of cell-cycle arrest, apoptosis, and autophagy in culture (PMID: 31217744). | 31217744 |
KIT N822K | acute myeloid leukemia | predicted - sensitive | Sunitinib | Preclinical - Cell culture | Actionable | In a preclinical study, Sutent (sunitinib) inhibited proliferation of acute myeloid leukemia cells harboring KIT N822K in culture (PMID: 31085175). | 31085175 |
KIT N822K | Advanced Solid Tumor | predicted - sensitive | Sunitinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT N822K were more sensitive to treatment with Sutent (sunitinib) in culture compared to Gleevec (imatinib), demonstrating decreased cell proliferation (PMID: 24205792). | 24205792 |
KIT N822K | thymus squamous cell carcinoma | predicted - sensitive | Avapritinib | Case Reports/Case Series | Actionable | In a clinical case study, Ayvakit (avapritinib) resulted in stable disease in a patient with thymus squamous cell carcinoma harboring KIT N822K (PMID: 35820244). | 35820244 |
KIT N822K | acute myeloid leukemia | sensitive | Avapritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Ayvakit (avapritinib) inhibited Kit phosphorylation and proliferation of acute myeloid leukemia cells harboring KIT N822K in culture (PMID: 29093181). | 29093181 |
KIT N822K | mucosal melanoma | predicted - sensitive | Avapritinib | Case Reports/Case Series | Actionable | In a clinical case study, Ayvakit (avapritinib) resulted in a partial response in extracranial lesions and stable disease in the central nervous lesions that lasted for 11 months in a patient with mucosal melanoma harboring KIT N822K (PMID: 35820244). | 35820244 |
KIT N822K | Advanced Solid Tumor | predicted - sensitive | Flumatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT N822K were more sensitive to treatment with Flumatinib in culture compared to Gleevec (imatinib), demonstrating decreased cell proliferation (PMID: 24205792). | 24205792 |
KIT N822K | acute myeloid leukemia | sensitive | Ripretinib | Preclinical - Pdx | Actionable | In a preclinical study, Qinlock (ripretinib) induced tumor regression in a patient-derived xenograft (PDX) model of acute myeloid leukemia harboring KIT N822K (Cancer Res 2015;75(15 Suppl):Abstract nr 2690). | detail... |
KIT N822K | acute myeloid leukemia | sensitive | Ripretinib | Preclinical - Cell culture | Actionable | In a preclinical study, Qinlock (ripretinib) inhibited proliferation of acute myeloid leukemia cells harboring KIT N822K in culture (PMID: 31085175). | 31085175 |
KIT N822K | acute myeloid leukemia | sensitive | BPR1J373 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, an acute myeloid leukemia cell line harboring KIT N822K demonstrated sensitivity to treatment with BPR1J373, showing inhibition of Kit phosphorylation and apoptotic induction in culture, and tumor regression in xenograft models (PMID: 27512117). | 27512117 |
KIT N822K | acute myeloid leukemia | decreased response | RMC-4550 | Preclinical - Cell culture | Actionable | In a preclinical study, acute myeloid leukemia cell lines harboring KIT N822K demonstrated decreased sensitivity to RMC-4550 treatment compared to cell lines harboring FLT3 ITD in culture (PMID: 37992684). | 37992684 |
KIT N822K | acute myeloid leukemia | sensitive | Trametinib + Venetoclax | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Venclexta (venetoclax) and Mekinist (trametinib) synergistically inhibited proliferation in acute myeloid leukemia cell lines harboring KIT N822K in culture (PMID: 37992684). | 37992684 |
KIT N822K | acute myeloid leukemia | sensitive | RMC-4550 + Venetoclax | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of RMC-4550 and Venclexta (venetoclax) synergistically inhibited viability and induced apoptosis in an acute myeloid leukemia cell line harboring KIT N822K in culture, and reduced tumor burden and improved survival in a cell line xenograft model (PMID: 37992684). | 37992684 |