货号	规格	价格	上海	北京	珠海	重庆	武汉
S87777-1mg买3赠1	98.70%	￥200.00 S87777-1mg ￥200.00 现货（买3赠1）	9 9	-	-	-	-
S87777-5mg买3赠1	98.70%	￥610.00 S87777-5mg ￥610.00 现货（买3赠1）	6 6	-	-	-	-
S87777-10mg买3赠1	98.70%	￥980.00 S87777-10mg ￥980.00 现货（买3赠1）	6 6	-	-	-	-
S87777-25mg促销	98.70%	￥1900.00 ￥1520.00 S87777-25mg ￥1520.00 现货	5 5	-	-	-	-
S87777-50mg促销	≥98%	￥3600.00 ￥2880.00 S87777-50mg ￥2880.00 2-3天	0 货期：2-3天	-	-	-	-
S87777-100mg促销	≥98%	￥6240.00 ￥4990.00 S87777-100mg ￥4990.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

BPR1J-097 Hydrochloride is a novel and potent FLT3 inhibitor with an IC50 of 11 nM.

靶点：

IC50: 11 nM (FLT3);FLT

体外研究：

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

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 mm3. 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

参考文献：

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.

溶解性：

Soluble in DMSO、H2O

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.936 ml	9.678 ml	19.357 ml
5 mM	0.387 ml	1.936 ml	3.871 ml
10 mM	0.194 ml	0.968 ml	1.936 ml
50 mM	0.039 ml	0.194 ml	0.387 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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