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| | 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 | | EINECS: | | | Product Categories: | | | 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 882370 Preparation Products And Raw materials |
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