BPR1J-097

BPR1J-097

中文名称BPR1J-097
中文同义词化合物BPR1J-097;PERFEMIKER]BPR1J-097,98%
英文名称BPR1J-097
英文同义词BPR1J-097;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;N-[5-(3-Benzenesulfonamidophenyl)-1H-pyrazol-3-yl]-4-(4-methylpiperazin-1-yl)benzamide;Benzamide, 4-(4-methyl-1-piperazinyl)-N-[5-[3-[(phenylsulfonyl)amino]phenyl]-1H-pyrazol-3-yl]-;BPR1J-097 hydrochloride;CS-2356;CS-2096
CAS号1327167-19-0
分子式C27H28N6O3S
分子量516.61
EINECS号
相关类别小分子抑制剂;小分子抑制剂,天然产物;抑制剂;标准品;Inhibitors
Mol文件1327167-19-0.mol
结构式BPR1J-097 结构式

BPR1J-097 性质

熔点247-248 °C
密度1.368±0.06 g/cm3(Predicted)
储存条件Store at -20°C
溶解度DMSO:10.0(最大浓度 mg/mL);19.36(最大浓度 mM)
DMF:30.0(最大浓度 mg/mL);58.07(最大浓度 mM)
DMF:PBS ( pH 7.2) (1:6):0.14(最大浓度 mg/mL);0.27(最大浓度 mM)
形态结晶固体
酸度系数(pKa)8.17±0.10(Predicted)

BPR1J-097 用途与合成方法

BPR1J-097 Hydrochloride 是一个新型且强效的 FLT3 抑制剂,其 IC50 值为 11 nM。

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.

安全信息

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/01/25HY-13537ABPR1J-097
BPR1J-097 Hydrochloride
1327167-19-02mg500元
2024/01/25HY-13537ABPR1J-097
BPR1J-097 Hydrochloride
1327167-19-05mg700元

BPR1J-097 上下游产品信息

"BPR1J-097"相关产品信息
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