1327167-19-0
基本信息
CS-2096
BPR1J-097
BPR1J-097 hydrochloride
BPR1J-097
BPR1J 097
BPR1J097
N-[5-(3-Benzenesulfonamidophenyl)-1H-pyrazol-3-yl]-4-(4-methylpiperazin-1-yl)benzamide
4-(4-methylpiperazin-1-yl)-N-(5-(3-(phenylsulfonamido)phenyl)-1H-pyrazol-3-yl)benzamide
N-(3-(3-[(phenylsulfonyl)amino]phenyl)-1H-pyrazol-5-yl)-4-(4-methylpiperazino) benzamide
Benzamide, 4-(4-methyl-1-piperazinyl)-N-[5-[3-[(phenylsulfonyl)amino]phenyl]-1H-pyrazol-3-yl]-
物理化学性质
| 熔点 | 247-248 °C |
| 密度 | 1.368±0.06 g/cm3(Predicted) |
| 储存条件 | -20°C储存 |
| 溶解度 | DMSO:10.0(Max Conc. mg/mL);19.36(Max Conc. mM) DMF:30.0(Max Conc. mg/mL);58.07(Max Conc. mM) DMF:PBS (pH 7.2) (1:6):0.14(Max Conc. mg/mL);0.27(Max Conc. mM) |
| 酸度系数(pKa) | 8.17±0.10(Predicted) |
| 形态 | 结晶固体 |
| 颜色 | White to off-white |
安全数据
| 危险性符号(GHS) |  GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H302-H315-H320-H335 |
| 防范说明 | P261-P280-P301+P312-P302+P352-P305+P351+P338 |
常见问题列表
IC50: 11 nM (FLT3)
BPR1J-097 Hydrochloride is a novel and potent FLT3 inhibitor with an IC 50 of 11nM. Phosphorylation of all FLT3-WT, FLT3-IDT, and FLT3-D835Y are inhibited by BPR1J-097 Hydrochloride at a concentration as low as 10 nM. BPR1J-097 Hydrochloride suppresses the phosphorylation of FLT3 and STAT5 in a dose-dependent manner. The IC 50 values of BPR1J-097 Hydrochloride on MOLM-13 and MV4-11 cells are 21±7 and 46±14 nM, respectively. The emergence of active caspase-3 is observed in MOLM-13 cells treated with BPR1J-097 Hydrochloride at 10 nM. The effect of BPR1J-097 Hydrochloride seems to be weaker in MV4-11 cells as caspase-3 is not evident until 100 nM of BPR1J-097 Hydrochloride is applied to treat cells.
After i.v. administration of mice with BPR1J-097 Hydrochloride at two cycles of 10 or 25 mg/kg, a clear dose-dependent anti-tumour effect is observed. Tumours in mice treated with BPR1J-097 Hydrochloride (25 mg/kg per day) stop growing. BPR1J-097 Hydrochloride (25 mg/kg) shows a significant tumour shrinkage effect on the subcutaneously growing MOLM-13 tumours in a size of >2000 mm 3 . BPR1J-097 Hydrochloride (10 and 25 mg/kg) also produces a dose-dependent growth reduction and shrinkage of another model using MV4-11 cells. It is noted that a prolonged disappearance of MV4-11 tumours is observed in mice treated with BPR1J-097 Hydrochloride at 25 mg/kg. There is little (3%) or no body weight loss of BPR1J-097 Hydrochloride-treated nude mice during the observation periods in these in vivo studies.