BI 882370
BI 882370 Basic information
- Product Name:
- BI 882370
- Synonyms:
-
- BI 882370
- BI882370;BI-882370
- 1-Propanesulfonamide, N-[3-[5-[(1-ethyl-4-piperidinyl)methylamino]-3-(5-pyrimidinyl)-1H-pyrrolo[3,2-b]pyridin-1-yl]-2,4-difluorophenyl]-
- CS-2615
- BI-882370,Raf,BI882370,inhibit,Inhibitor,Raf kinases,BI 882370
- N-(3-(5-((1-Ethylpiperidin-4-yl)(methyl)amino)-3-(pyrimidin-5-yl)-1H-pyrrolo[3,2-b]pyridin-1-yl)-2,4-difluorophenyl)propane-1-sulfonamide
- CAS:
- 1392429-79-6
- MF:
- C28H33F2N7O2S
- MW:
- 569.67
- Mol File:
- 1392429-79-6.mol
BI 882370 Chemical Properties
- Boiling point:
- 649.6±65.0 °C(Predicted)
- Density
- 1.37±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:5.0(Max Conc. mg/mL);8.78(Max Conc. mM)
- form
- A crystalline solid
- pka
- 5.48±0.10(Predicted)
- color
- Off-white to gray
BI 882370 Usage And Synthesis
Description
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. 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 , induces tumor regression in an A375 melanoma mouse xenograft model with no resistance developing within three or five weeks, respectively.
BI 882370Supplier
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