A RAF inhibitor (IC50s = 0.8

BI-882370 – 10 mg

Brand:
Cayman
CAS:
1392429-79-6
Storage:
-20
UN-No:
Non-Hazardous - /

BI-882370 is an orally bioavailable RAF inhibitor with IC50 values of 0.8, 0.8, and 0.6 nM for B-RAFV600E, wild-type B-RAF, and C-RAF in the DFG-out inactive conformation, respectively.{42482} It is selective for RAF over a panel of kinases, including LCK, KIT, Src, LYNA, LYNB, and PDGFR (IC50s = 49, 415, 485, 750, 715, and 1,220 nM, respectively). It inhibits proliferation of human B-RAF-mutant melanoma cells when used at concentrations ranging from 1 to 10 nM. It reduces tumor growth in multiple B-RAF-mutant melanoma and colorectal carcinoma mouse xenograft models when administered at a dose of 25 mg/kg twice per day. BI-882370, alone and in combination with trametinib (Item No. 16292), induces tumor regression in an A375 melanoma mouse xenograft model with no resistance developing within three or five weeks, respectively.  

 

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SKU: 24273 - 10 mg Category:

Description

A RAF inhibitor (IC50s = 0.8, 0.8, and 0.6 nM for B-RAFV600E, wild-type B-RAF, and C-RAF in the DFG-out inactive conformation, respectively); selective for RAF over a panel of kinases, including LCK, KIT, Src, LYNA, LYNB, and PDGFR (IC50s = 49, 415, 485, 750, 715, and 1,220 nM, respectively); inhibits proliferation of human B-RAF-mutant melanoma cells at 1-10 nM; reduces tumor growth in multiple B-RAF-mutant melanoma and colorectal carcinoma mouse xenograft models at 25 mg/kg twice per day

Formal name: N-[3-[5-[(1-ethyl-4-piperidinyl)methylamino]-3-(5-pyrimidinyl)-1H-pyrrolo[3,2-b]pyridin-1-yl]-2,4-difluorophenyl]-1-propanesulfonamide

Synonyms: 

Molecular weight: 569.7

CAS: 1392429-79-6

Purity: ≥95%

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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