Molecular Profile Detail

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Profile Name MAP2K1 F53L
Gene Variant Detail

MAP2K1 F53L (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 F53L colorectal cancer sensitive MEK inhibitor (Pan) MEK1 Inhibitor Trametinib Preclinical Actionable In a preclinical study, a colorectal cancer cell line harboring MAP2K1 F53L demonstrated sensitivity to Mekinist (trametinib) in culture, resulting in decreased cell viability (PMID: 26582713). 26582713
MAP2K1 F53L colorectal cancer resistant Cetuximab Preclinical - Cell culture Actionable In a preclinical study, expression of MAP2K1 F53L conferred resistance to Erbitux (cetuximab) in colorectal cancer cells in culture (PMID: 28179366). 28179366
MAP2K1 F53L colorectal cancer sensitive MEK inhibitor (Pan) MEK1 Inhibitor Cetuximab + Trametinib Preclinical - Cell culture Actionable In a preclinical study, the combination of Erbitux (cetuximab) and Mekinist (trametinib) decreased viability of colorectal cancer cells harboring MAP2K1 F53L in culture (PMID: 28179366). 28179366
MAP2K1 F53L Advanced Solid Tumor sensitive MEK inhibitor (Pan) MEK1 Inhibitor Selumetinib Preclinical - Cell culture Actionable In a preclinical study, Map2k1 F53L displayed sensitivity to the Mek inhibitor, Selumetinib (AZD6244), as demonstrated by reversal of active Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
MAP2K1 F53L Advanced Solid Tumor sensitive PLX4720 Preclinical - Cell culture Actionable In a preclinical study, Map2k1 F53L displayed sensitivity to the Braf inhibitor, PLX4720, as demonstrated by reversal of active Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
MAP2K1 F53L Advanced Solid Tumor resistant MEK1 Inhibitor PD98059 Preclinical - Cell culture Actionable In a preclinical study, Map2k1 F53L displayed resistance to the Mek inhibitor, PD98059, as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
MAP2K1 F53L Advanced Solid Tumor resistant Regorafenib Preclinical - Cell culture Actionable In a preclinical study, Map2k1 F53L displayed resistance to Stivarga (regorafenib; BAY 73-4506), as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
MAP2K1 F53L Advanced Solid Tumor resistant GDC0879 Preclinical - Cell culture Actionable In a preclinical study, Map2k1 F53L displayed resistance to the Braf inhibitor, GDC-0879, as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
MAP2K1 F53L Advanced Solid Tumor resistant MEK inhibitor (Pan) MEK1 Inhibitor AZD8330 Preclinical - Cell culture Actionable In a preclinical study, Map2k1 F53L displayed resistance to the Mek inhibitor, AZD8330, as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
MAP2K1 F53L histiocytic sarcoma predicted - sensitive MEK inhibitor (Pan) MEK1 Inhibitor Trametinib Case Reports/Case Series Actionable In a clinical case study, Mekinist (trametinib) treatment resulted in resolution of symptoms within 3 days and a durable complete response for over 2 years in a patient with histiocytic sarcoma harboring MAP2K1 F53L (PMID: 29768143). 29768143
MAP2K1 F53L Advanced Solid Tumor sensitive MEK inhibitor (Pan) MEK1 Inhibitor Selumetinib Preclinical - Cell culture Actionable In a preclinical study, Koselugo (selumetinib) inhibited colony formation of transformed cells expressing MAP2K1 F53L in culture (PMID: 25351745). 25351745
MAP2K1 F53L 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 F53L in culture (PMID: 36442478). 36442478
MAP2K1 F53L Advanced Solid Tumor sensitive MEK inhibitor (Pan) MEK1 Inhibitor Trametinib Preclinical - Biochemical Actionable In a preclinical study, Mekinist (trametinib) inhibited Erk phosphorylation in transformed cells expressing MAP2K1 F53L in culture (PMID: 32641410). 32641410