FN-1501 is a potent a FLT3/CDKs kinase inhibitor with potential high efficiency against acute myelocytic leukemia (AML). FN-1501, which possesses potent inhibitory activities against FLT3, CDK2, CDK4, and CDK6 with IC50 in the nanomolar range, shows antiproliferative activities against MV4-11 cells ( 0.008 μM), which correlates with the suppression of retinoblastoma phosphorylation, FLT3, ERK, AKT, and STAT5 and the onset of apoptosis. Acute-toxicity studies in mice show that FN-1501 ( 186 mg/kg) is safer than AT7519 (32 mg/kg). In MV4-11 xenografts in a nude-mouse model, FN-1501 can induce tumor regression at the dose of 15 mg/kg, which is more efficient than cytarabine (50 mg/kg). References: Wang Y, Zhi Y, Jin Q, Lu S, Lin G, Yuan H, Yang T, Wang Z, Yao C, Ling J, Guo H, Li T, Jin J, Li B, Zhang L, Chen Y, Lu T. Discovery of 4-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazole-3-carboxamide (FN-1501), as a FLT3/CDKs kinase inhibitor with potential high efficiency against acute myelocytic leukemia (AML). J Med Chem. 2018 Jan 22. doi: 10.1021/acs.jmedchem.7b01261. [Epub ahead of print] PubMed PMID: 29357250.

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CAS：1429515-59-2