貨號(hào)	產(chǎn)品規(guī)格	價(jià)格(RMB)	庫(kù)存（上海）	北京	武漢	南京
S80323-1mg	≥98%	￥200.00元	5	-	-	-
S80323-5mg	≥98%	￥700.00元	6	-	-	-
S80323-10mg	≥98%	￥960.00元	6	-	-	-
S80323-25mg	≥98%	￥1800.00元	6	-	-	-
S80323-50mg	≥98%	￥2800.00元	5	-	-	-
S80323-100mg	≥98%	￥4400.00元	2	-	-	-

產(chǎn)品介紹

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

產(chǎn)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

靶點(diǎn)：

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

體內(nèi)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)

參考文獻(xiàn)：

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

保存條件：

-20℃

配置溶液濃度參考：

	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：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻(xiàn)

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AMG 925