BI-882370 – 5 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.  

 

Available on backorder

SKU: 24273 - 5 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