BPR1J-340
CAS 1395051-72-5 MFCD495051725
化学结构图
SMILES: CCc1cc(NC(=O)NCc2ccc(-c3cc(NC(=O)c4ccc(CN5CCN(C)CC5)cc4)[nH]n3)cc2)no1
化学属性
| Mol. Weight | 542.63206 |
|---|---|
| Appearance | white solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name | BPR1J-340 |
|---|---|
| Formula | C29H34N8O3 |
| Synonym | BPR1J340; BPR1J 340; BPR1J-340. |
| IUPAC Name | N-(3-(4-((3-(5-ethylisoxazol-3-yl)ureido)methyl)phenyl)-1H-pyrazol-5-yl)-4-((4-methylpiperazin-1-yl)methyl)benzamide |
| InChIKey | VHFDRDHFZFLAAT-UHFFFAOYSA-N |
| InChI | InChI=1S/C29H34N8O3/c1-3-24-16-27(35-40-24)32-29(39)30-18-20-4-8-22(9-5-20)25-17-26(34-33-25)31-28(38)23-10-6-21(7-11-23)19-37-14-12-36(2)13-15-37/h4-11,16-17H,3,12-15,18-19H2,1-2H3,(H2,30,32,35,39)(H2,31,33,34,38) |
| Canonical SMILES | O=C(NC1=CC(C2=CC=C(CNC(NC3=NOC(CC)=C3)=O)C=C2)=NN1)C4=CC=C(CN5CCN(C)CC5)C=C4 |
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产品应用
- BPR1J-340 is a potent and selective FLT3 inhibitor with potential anticancer activity. BPR1J-340 was identified as a novel potent FLT3 inhibitor by biochemical kinase activity (IC50 approximately 25 nM) and cellular proliferation (GC50 approximately 5 nM) assays. BPR1J-340 inhibited the phosphorylation of FLT3 and STAT5 and triggered apoptosis in FLT3-ITD(+) AML cells. The pharmacokinetic parameters of BPR1J-340 in rats were determined. BPR1J-340 also demonstrated pronounced tumor growth inhibition and regression in FLT3-ITD(+) AML murine xenograft models. The combination treatment of the HDAC inhibitor vorinostat (SAHA) with BPR1J-340 synergistically induced apoptosis via Mcl-1 down-regulation in MOLM-13 AML cells, indicating that the combination of selective FLT3 kinase inhibitors and HDAC inhibitors could exhibit clinical benefit in AML therapy.
