10-4112
Avutometinib
Size
£197.00
- SKU:
- 10-4112
- Additional Names:
- CH5126766|CKI-27|R-7304|RG-7304|RO5126766|VS-6766
- Physical State:
- Solid
- Molecular Weight:
- 471.46
- Purity:
- >98%
- Purification:
- HPLC Purified
- Storage Conditions:
- -20[o]C
- Supplier:
- Focus Biomolecules
- CAS Number:
- 946128-88-7
- Immunogen:
- Kinase
- Extra Details:
- 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
- Shipping Conditions:
- Ambient