MRTX-EX185 formic 是负载 GDP 的 KRAS 和 KRAS(G12D) 的有效抑制剂,对 KRAS(G12D) 的 IC50 值为 90 nM。MRTX-EX185 formic 还结合 GDP 负载的 HRAS。
生物活性
MRTX-EX185 formic is a potent inhibitor of GDP-loaded KRAS and KRAS(G12D), with an IC 50 of 90 nM for KRAS(G12D). MRTX-EX185 formic also binds GDP-loaded HRAS.
性状
Solid
IC50 & Target[1][2]
KRas G12D 90 nM (IC50)
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
参考文献
[1]. Vasta JD, et, al. KRAS is vulnerable to reversible switch-II pocket engagement in cells. Nat Chem Biol. 2022 Mar 21.
溶解度数据
In Vitro: DMSO : 125 mg/mL (204.69 mM; Need ultrasonic)配制储备液