CAS NO: | 1392429-79-6 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | BI-882370 is a potent and selectiveRAFkinase inhibitor that binds to the ATP binding site of the kinase positioned in the DFG-out (inactive) conformation of theBRAFkinase. BI-882370 (BI 882370) inhibits the oncogenicBRAFV600E-mutant, the WTBRAFand CRAF kinases withIC50sof 0.4, 0.8, and 0.6 nM, respectively. BI-882370 also inhibitsSRCfamily kinases[1]. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | BI-882370 (0.9-6000 nM; 3 days) inhibits the BRAF-mutant human melanoma and colorectal cancer cells proliferation with a EC50range of 1-10 nM[1].BI 882370 (0.1-100 nM, 0.1-3000 nM; 2 hours) results in a reduction of p-MEK1/2, p-ERK1/2 and cyclin D1/D2 expression in BRAFV600E-mutant A375 cells; induces phosphorylation of MEK1/2 and enhanced phosphorylation of ERK1/2 in WT BRO cells (3-300 nM)[1].BI 882370 (0.1-100 nM, 0.1-3000 nM; 24 hours) suppresses cyclin D1/D2 expression, induces Kip1/p27 expression at concentrations of 1 nM or higher in BRAFV600E-mutant A375 cells, expression of cyclins D1/D2 or Kip1/p27 is not affected in WT BRO cells[1]. Cell Proliferation Assay[1]
Western Blot Analysis[1]
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体内研究 (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].
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分子量 | 569.67 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C28H33F2N7O2S | ||||||||||||||||
CAS 号 | 1392429-79-6 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 5 mg/mL(8.78 mM;ultrasonic and warming and heat to 60℃) H2O :< 0.1 mg/mL(insoluble) 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |