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CAS No. : 1392429-79-6
MCE 国际站:BI-882370
产品活性:BI-882370 是一种高效选择性的 RAF 激酶抑制剂,其结合位于 BRAF 激酶的 DFG-out 无活性构象处 (ATP 结合位点)。 BI-882370 抑制 BRAFV600E-mutant, WT BRAF 和 CRAF 激酶的 IC50 值分别为 0.4,0.8 和 0.6 nM。BI-882370 也可以抑制 SRC 家族激酶。
研究领域:MAPK/ERK Pathway
作用靶点:Raf
In Vitro: BI-882370 (0.9-6000 nM; 3 days) inhibits the BRAF-mutant human melanoma and colorectal cancer cells proliferation with a EC50 range of 1-10 nM.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).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.
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.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.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.
相关产品:Bioactive Compound Library Plus | Immunology/Inflammation Compound Library | Kinase Inhibitor Library | MAPK Compound Library | Anti-Cancer Compound Library | Oxygen Sensing Compound Library | Ferroptosis Compound Library | Glutamine Metabolism Compound Library | Anti-Lung Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Obesity Compound Library | Anti-Liver Cancer Compound Library | Anti-Colorectal Cancer Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | B-Raf IN 2 | Avutometinib | Sorafenib-d4 | AZ 628 | B-Raf IN 7 | Antitumor agent-60 | Sorafenib Tosylate | Dabrafenib Mesylate | SB-682330A | Belvarafenib TFA | L-779450 | B-Raf IN 9 | Debromohymenialdisine | Raf inhibitor 1 | TBAP-001 | RRD-251 | Encorafenib-13C,d3 | PLX-4720 | TAK-632 | Norartocarpetin | Encorafenib | LUT014 | Rineterkib | Raf inhibitor 2 | Regorafenib monohydrate | AD57 | AD80
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货号: HY-107779
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