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10-4112

Avutometinib

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£197.00

SKU:
10-4112
Zusätzliche Namen:
CH5126766|CKI-27|R-7304|RG-7304|RO5126766|VS-6766
Physischer Zustand:
Solid
Molekulargewicht:
471.46
Reinheit:
>98%
Aufreinigung:
HPLC Purified
Lagerbedingungen:
-20[o]C
Hersteller:
Focus Biomolecules
CAS Number:
946128-88-7
Immunogen:
Kinase
Weitere 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
Versandbedingungen:
Ambient