BPR1J-097 4-(4-甲基哌嗪-1-基)-N-(5-(3-(苯磺酰胺基)苯基)-1H-吡唑-3-基)苯甲酰胺
CAS 1327167-19-0 MFCD427167190
化学结构图
SMILES: CN1CCN(c2ccc(C(=O)Nc3cc(-c4cccc(NS(=O)(=O)c5ccccc5)c4)n[nH]3)cc2)CC1
化学属性
| Mol. Weight | 516.61 |
|---|---|
| Appearance | white solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name Translation | 4-(4-甲基哌嗪-1-基)-N-(5-(3-(苯磺酰胺基)苯基)-1H-吡唑-3-基)苯甲酰胺 |
|---|---|
| Chemical Name | BPR1J-097 |
| Formula | C27H28N6O3S |
| Synonym | BPR1J097; BPR1J-097; BPR1J 097; BPR1-J097; BPR1 J097; BPR1J097 |
| IUPAC Name | 4-(4-methylpiperazin-1-yl)-N-(3-(3-(phenylsulfonamido)phenyl)-1H-pyrazol-5-yl)benzamide. |
| InChIKey | RRKKHABFIOHAOI-UHFFFAOYSA-N |
| InChI | InChI=1S/C27H28N6O3S/c1-32-14-16-33(17-15-32)23-12-10-20(11-13-23)27(34)28-26-19-25(29-30-26)21-6-5-7-22(18-21)31-37(35,36)24-8-3-2-4-9-24/h2-13,18-19,31H,14-17H2,1H3,(H2,28,29,30,34) |
| Canonical SMILES | O=C(NC1=CC(C2=CC=CC(NS(=O)(C3=CC=CC=C3)=O)=C2)=NN1)C4=CC=C(N5CCN(C)CC5)C=C4 |
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产品应用
- BPR1J-097 is a novel small molecule FLT-3 inhibitor with promising in vivo anti-tumour activities. BPR1J-097 may be useful in AML treatments.IC50 of BPR1J-097 required to inhibit FLT3 kinase activity ranged from 1 to 10 nM, and the 50% growth inhibition concentrations (GC(50)s) were 21±7 and 46±14 nM for MOLM-13 and MV4-11 cells, respectively. BPR1J-097 inhibited FLT3/signal transducer and activator of transcription 5 phosphorylation and triggered apoptosis in FLT3-driven AML cells. BPR1J-097 also showed favourable pharmacokinetic property and pronounced dose-dependent tumour growth inhibition and regression in FLT3-driven AML murine xenograft models.
