Avutometinib
Product Specifications
Background
Avutometinib is a dual MEK/RAF inhibitor (IC50s: MEK = 160 nM; CRAF = 56 nM; BRAF = 19 nM; BRAF V600E = 8nM) .1 It directly inhibits unphosphorylated MEK without causing induction of MEK phosphorylation by RAF. The avutemetinib-MEK adduct is a dominant-negative inhibitor of RAF, stabilizing the MEK/RAF complex and locking in an inactive form. Avutometinib displayed efficacy across multiple RAS-mutated cancer cell lines and an SK-MEL-2 xenograft model.2 It displayed synergistic effects with eribulin against triple-negative breast cancer cell lines.3 Avutometinib also displayed efficacy in combination with the FAK inhibitor Defactinib in KRAS-mutated NSCLC cells.4
Conjugation
Unconjugated
Buffer
White solid
Storage Conditions
-20°C
Available Sizes
Frequently Asked Questions
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