bs-83753C

DATASHEET

Formulation White solid

Storage: -20°C

Product Information:

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

Description:

CAS Number: 946128-88-7 Chemical Name: 3-[[3-Fluoro-2-(methylsulfamoylamino)pyridin-4-yl]methyl]-4-methyl-7-pyrimidin-2-yloxychromen-2-one Molecular Weight: 471.46 Formula: C21H18FN5O5S Solubility: DMSO (>25 mg/ml) Physical Properties: White solid Purity: >98% by HPLC (NMR Conforms)