货号	规格	价格	上海	北京	珠海	重庆	武汉
S80323-1mg买3赠1	99.10%	￥200.00 S80323-1mg ￥200.00 现货（买3赠1）	5 5	-	-	-	-
S80323-5mg买3赠1	99.10%	￥700.00 S80323-5mg ￥700.00 现货（买3赠1）	6 6	-	-	-	-
S80323-10mg买3赠1	99.10%	￥960.00 S80323-10mg ￥960.00 现货（买3赠1）	6 6	-	-	-	-
S80323-25mg买3赠1	99.10%	￥1800.00 S80323-25mg ￥1800.00 现货（买3赠1）	6 6	-	-	-	-
S80323-50mg买3赠1	99.10%	￥2800.00 S80323-50mg ￥2800.00 现货（买3赠1）	5 5	-	-	-	-
S80323-100mg买3赠1	≥98%	￥4400.00 S80323-100mg ￥4400.00 现货（买3赠1）	2 2	-	-	-	-

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产品描述：

AMG 925 is a potent, selective, and orally available FLT3/CDK4 dual inhibitor with IC50s of 2±1 nM and 3±1 nM, respectively

靶点：

FLT3:2 nM (IC50);CDK4:3 nM (IC50);CDK6:8 nM (IC50);CDK2:375 nM (IC50);CDK1:1.9 μM (IC50);FLT;CDK

体内研究：

MOLM13 tumor-bearing mice are dosed twice daily by oral administration 6 hours apart with 12.5, 25, or 37.5 mg/kg AMG 925. Tumors are then harvested 3, 9, 12, and 24 hours after the first dose, and analyzed for levels of P-STAT5 and P-RB. Maximum inhibition of P-STAT5 and P-RB is achieved at 6 and 12 hours respectively at the 37.5 mg/kg dose of AMG 925. Interestingly, a rebound of P-STAT5 at 24 hours is observed, possibly as a result of compensational feedback. The pharmacodynamic responses of P-STAT5 and P-RB inhibition correlated with plasma concentrations of AMG 925. AMG 925 inhibits AML xenograft tumor growth by 96% to 99% without significant body weight loss. The antitumor activity of AMG 925 correlates with the inhibition of STAT5 and retinoblastoma protein (RB) phosphorylation, the pharmacodynamic markers for inhibition of FLT3 and CDK4, respectively. In addition, AMG 925 is also found to inhibit FLT3 mutants (e.g., D835Y) that are resistant to the current FLT3 inhibitors (e.g., AC220 and Sorafenib)

参考文献：

1. Keegan K, et al. Preclinical evaluation of AMG 925, a FLT3/CDK4 dual kinase inhibitor for treating acute myeloid leukemia. Mol Cancer Ther. 2014 Apr;13(4):880-9.

溶解性：

10 mM in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.121 ml	10.603 ml	21.206 ml
5 mM	0.424 ml	2.121 ml	4.241 ml
10 mM	0.212 ml	1.06 ml	2.121 ml
50 mM	0.042 ml	0.212 ml	0.424 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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