BPR1J-097

生物活性靶点体外研究体内研究 BPR1J-097 试剂级价格

BPR1J-097

CAS号:1327167-19-0
英文名:BPR1J-097
中文名:BPR1J-097
CBNumber:CB32667855
分子式:C27H28N6O3S
分子量:516.61
MOL File:1327167-19-0.mol

BPR1J-097化学性质

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(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)
形态 :A crystalline solid
酸度系数(pKa) :8.17±0.10(Predicted)
颜色 :White to off-white

BPR1J-097性质、用途与生产工艺

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

IC50: 11 nM (FLT3)
体外研究

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.
体内研究

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.