A potent inhibitor of B-RAF and C-RAF (IC50s = 0.4 and 0.5 nM

RAF709 – 1 mg

Brand:
Cayman
CAS:
1628838-42-5
Storage:
-20
UN-No:
Non-Hazardous - /

RAF709 is a potent inhibitor of B-RAF and C-RAF (IC50s = 0.4 and 0.5 nM, respectively).{37294} It is selective for RAF kinases exhibiting >99% inhibition of only B-RAF, B-RAFV600E, and C-RAF in a panel of 456 kinases. However, DDR1, DDR2, FRK, and PDGFRβ are also inhibited by >80% at a concentration of 1 μM. RAF709 inhibits phosphorylation of MEK and ERK (EC50s = 0.02 and 0.1 μM, respectively) with minimal paradoxical activation, stabilizes BRAF-CRAF dimers (EC50 = 0.8 μM), and reduces proliferation of Calu-6 RAS mutant cells (EC50 = 0.95 μM). In a Calu-6 mouse non-small cell lung cancer (NSCLC) xenograft model, RAF709 (10-200 mg/kg) reduces ERK phosphorylation and decreases tumor volume in a dose-dependent manner without affecting total body weight.  

 

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Description

A potent inhibitor of B-RAF and C-RAF (IC50s = 0.4 and 0.5 nM, respectively); selective for RAF kinases exhibiting >99% inhibition of only B-RAF, B-RAFV600E, and C-RAF in a panel of 456 kinases; DDR1, DDR2, FRK, and PDGFRβ are also inhibited by >80% at a concentration of 1 μM; inhibits phosphorylation of MEK and ERK (EC50s = 0.02 and 0.1 μM, respectively) with minimal paradoxical activation, stabilizes BRAF-CRAF dimers (EC50 = 0.8 μM), and reduces proliferation of Calu-6 RAS mutant cells (EC50 = 0.95 μM); reduces ERK phosphorylation and decreases tumor volume without affecting total body weight in a Calu-6 mouse NSCLC xenograft model when administered at doses ranging from 10-200 mg/kg

Formal name: N-[2-methyl-5′-(4-morpholinyl)-6′-[(tetrahydro-2H-pyran-4-yl)oxy][3,3′-bipyridin]-5-yl]-3-(trifluoromethyl)-benzamide

Synonyms: 

Molecular weight: 542.6

CAS: 1628838-42-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|RAS/RAF/MEK/ERK/MAPK||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|ERK/MAPK Signaling

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