BI 882370 manufacturers
- BI-882370
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- $36.00 / 1mg
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2025-09-22
- CAS:1392429-79-6
- Min. Order:
- Purity: 97.78%
- Supply Ability: 10g
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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;XP-102 | | CAS: | 1392429-79-6 | | MF: | C28H33F2N7O2S | | MW: | 569.67 | | EINECS: | | | Product Categories: | BI 882370 | | 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. | | Uses | BI-882370 is a potent and selective RAF kinase inhibitor that binds to the ATP binding site of the kinase positioned in the DFG-out (inactive) conformation of the BRAF kinase. BI-882370 (BI 882370) inhibits the oncogenic BRAFV600E-mutant, the WT BRAF and CRAF kinases with IC50s of 0.4, 0.8, and 0.6 nM, respectively. BI-882370 also inhibits SRC family kinases[1]. | | in vivo | BI-882370 (deliver orally; 25 mg/kg, 50 mg/kg; twice daily; 2 weeks) is efficacious in multiple mouse models of BRAF-mutant melanomas and colorectal carcinomas, shows superior efficacy compared with Vemurafenib, Dabrafenib, or Trametinib[1].
BI-882370 (deliver orally; 25 mg/kg; twice daily; 40 days) developes resistance within 3 weeks, but resistance is not observed during 5 weeks of second-line therapy in combination with trametinib[1].
BI-882370 (deliver orally; 60 mg/kg; once daily; 2 weeks) indicates lack of toxicity in terms of clinical chemistry, hematology, pathology, and toxicogenomics in rats[1]. | Animal Model: | Human melanoma xenografts in nude mice with BRAF-mutant melanomas and colorectal carcinomas cells (A375, COLO 205; G-361, HT-29 cells)[1] | | Dosage: | 25 mg/kg; 50 mg/kg | | Administration: | Deliver orally; 25 mg/kg, 50 mg/kg; twice daily; 2 weeks | | Result: | Regressed tumors partially, upon discontinuation, tumor regrowth was markedly delayed. |
| | IC 50 | Braf: 0.6 nM (IC50); c-Raf: 0.8 nM (IC50); BRafV600E: 0.4 nM (IC50) | | References | [1] Waizenegger IC, et al. A Novel RAF Kinase Inhibitor with DFG-Out-Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation. Mol Cancer Ther. 2016 Mar;15(3):354-65. DOI:10.1158/1535-7163.MCT-15-0617 |
| | BI 882370 Preparation Products And Raw materials |
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