产品说明书

Gartisertib

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Chemical Structure| 1613191-99-3 同义名 : VX-803;M4344;Gartisertibum;ATR inhibitor 2
CAS号 : 1613191-99-3
货号 : A722379
分子式 : C25H29F2N9O3
纯度 : 98%
分子量 : 541.553
MDL号 : MFCD31803930
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(46.16 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Gartisertib (VX-803) is an orally active, ATP-competitive, and selective inhibitor of ATR, with a Ki value of <150 pM. It effectively suppresses ATR-driven phosphorylation of checkpoint kinase-1 (Chk1) with an IC50 of 8 nM. It also demonstrates significant antitumor activity [1][2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.85mL

0.37mL

0.18mL

9.23mL

1.85mL

0.92mL

18.47mL

3.69mL

1.85mL
参考文献

[1]Frank T. Zenke, et al. Abstract 369: Antitumor activity of M4344, a potent and selective ATR inhibitor, in monotherapy and combination therapy. Experimental and Molecular Therapeutics.

[2]Gorecki L, et al. Discovery of ATR kinase inhibitor berzosertib (VX-970, M6620): Clinical candidate for cancer therapy. Pharmacol Ther. 2020 Feb 26:107518.