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

BPR1J-097 Hydrochloride is a novel and potent FLT3 inhibitor with an IC 50 of 11?nM.

Solid

IC50: 11 nM (FLT3)

BPR1J-097 Hydrochloride is a novel and potent FLT3 inhibitor with an IC50 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 IC50 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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. 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. has not independe

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[1]. Lin WH, et al. BPR1J-097, a novel FLT3 kinase inhibitor, exerts potent inhibitory activity against AML. Br J Cancer. 2012 Jan 31;106(3):475-81.

In Vitro: DMSO : 6 mg/mL (10.85 mM; Need ultrasonic and warming)H₂O : 2 mg/mL (3.62 mM; Need ultrasonic)配制储备液