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KI0587BPR1J-09720 mg$945

Chemical Characteristic

Product NameBPR1J-097
CAS No.1327167-19-0
Molecular Weight 516.61
FormulaC27H28N6O3S
Chemical Name4-(4-methylpiperazin-1-yl)-N-(5-(3-(phenylsulfonamido)phenyl)-1H-pyrazol-3-yl)benzamide
SmilesC(=O)(c1ccc(cc1)N1CCN(CC1)C)Nc1n[nH]c(c1)c1cc(ccc1)NS(=O)(=O)c1ccccc1
Chemical Structure

Biological activities

BPR1J-097 is a novel fms-like tyrosine 3 (FLT3) kinase inhibitor. BPR1J-097 potently inhibits wild-type FLT3 (FLT3-WT) and FLT3-D835Y with IC50 of 11 and 3 nM, respectively. The IC50 of BPR1J-097 against FLT1 (VEGFR1) and KDR (VEGFR2) is 0.2 and 0.1 μM, respectively. And the IC50 of BPR1J-097 against Aurora A kinase and Aurora B kinase is 0.3 and 0.8 μM, respectively. BPR1J-097 inhibits the phosphorylation of FLT3 (FLT3-WT, FLT3-ITD and FLT3-D835Y) and STAT5 in HEK293T cells. The 50% growth inhibition concentrations (GC50s) of BPR1J-097 against MOLM-13 and MV4-11 cells are 21 and 46 nM, respectively. BPR1J-097 induces apoptosis in FLT3-ITD leukaemic cells. BPR1J-097 also shows favourable pharmacokinetic property and pronounced dose-dependent tumour growth inhibition and regression in FLT3-driven acute myeloid leukaemia (AML) murine xenograft models.[1]

References

[1] Lin WH, et al. BPR1J-097, a novel FLT3 kinase inhibitor, exerts potent inhibitory activity against AML. Br J Cancer. 2012, 106(3): 475-481.

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