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Profile Name MAP2K1 F129L
Gene Variant Detail

MAP2K1 F129L (gain of function)

Relevant Treatment Approaches MEK inhibitor (Pan) MEK1 Inhibitor

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Molecular Profile Indication/Tumor Type Response Type Relevant Treatment Approaches Therapy Name Approval Status Evidence Type Efficacy Evidence References
MAP2K1 F129L colorectal cancer sensitive MEK inhibitor (Pan) RO4927350 Preclinical - Cell line xenograft Actionable In a preclinical study, a colorectal cancer cell line harboring MAP2K1 F129L demonstrated sensitivity to treatment with RO4927350 in culture and in cell line xenograft models, demonstrating inhibition of tumor growth (PMID: 21705440). 21705440
MAP2K1 F129L Advanced Solid Tumor sensitive MEK inhibitor (Pan) MEK1 Inhibitor Selumetinib Preclinical - Cell culture Actionable In a preclinical study, Map2k1 F129L displayed sensitivity to the Mek inhibitor, Selumetinib (AZD6244), as demonstrated by reversal of active Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
MAP2K1 F129L Advanced Solid Tumor sensitive PLX4720 Preclinical - Cell culture Actionable In a preclinical study, Map2k1 F129L displayed sensitivity to the Braf inhibitor, PLX4720, as demonstrated by reversal of active Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
MAP2K1 F129L Advanced Solid Tumor resistant MEK1 Inhibitor PD98059 Preclinical - Cell culture Actionable In a preclinical study, Map2k1 F129L displayed resistance to the Mek inhibitor, PD98059, as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
MAP2K1 F129L Advanced Solid Tumor resistant Regorafenib Preclinical - Cell culture Actionable In a preclinical study, Map2k1 F129L displayed resistance to Stivarga (regorafenib; BAY 73-4506), as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
MAP2K1 F129L Advanced Solid Tumor resistant GDC0879 Preclinical - Cell culture Actionable In a preclinical study, Map2k1 F129L displayed resistance to the Braf inhibitor, GDC-0879, as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
MAP2K1 F129L Advanced Solid Tumor resistant MEK inhibitor (Pan) MEK1 Inhibitor AZD8330 Preclinical - Cell culture Actionable In a preclinical study, Map2k1 F129L displayed resistance to the Mek inhibitor, AZD8330, as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
MAP2K1 F129L Advanced Solid Tumor sensitive MEK inhibitor (Pan) MEK1 Inhibitor Trametinib Preclinical - Cell culture Actionable In a preclinical study, Mekinist (trametinib) inhibited viability of a transformed cell line expressing MAP2K1 F129L in culture (PMID: 36442478). 36442478
MAP2K1 F129L ovarian serous carcinoma resistant MEK inhibitor (Pan) MEK1 Inhibitor Trametinib Preclinical - Cell culture Actionable In a preclinical study, MAP2K1 F129L was identified in a low grade serous ovarian cancer cell line that developed resistance to treatment with Mekinist (trametinib) in culture (PMID: 36198031). 36198031
MAP2K1 F129L ovarian serous carcinoma resistant MEK inhibitor (Pan) MEK1 Inhibitor Selumetinib Preclinical - Cell culture Actionable In a preclinical study, a low grade serous ovarian cancer cell line harboring MAP2K1 F129L was resistant to treatment with Koselugo (selumetinib) in culture (PMID: 36198031). 36198031
MAP2K1 F129L ovarian serous carcinoma resistant MEK inhibitor (Pan) MEK1 Inhibitor Binimetinib Preclinical - Cell culture Actionable In a preclinical study, a low grade serous ovarian cancer cell line harboring MAP2K1 F129L was resistant to treatment with Mektovi (binimetinib) in culture (PMID: 36198031). 36198031
MAP2K1 F129L ovarian serous carcinoma resistant MEK inhibitor (Pan) MEK1 Inhibitor Refametinib Preclinical - Cell culture Actionable In a preclinical study, a low grade serous ovarian cancer cell line harboring MAP2K1 F129L was resistant to treatment with Refametinib (BAY86-9766) in culture (PMID: 36198031). 36198031