产品说明书

MRTX1133

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Chemical Structure| 2621928-55-8 同义名 : -
CAS号 : 2621928-55-8
货号 : A1501270
分子式 : C33H31F3N6O2
纯度 : 98% LC
分子量 : 600.634
MDL号 : MFCD34567005
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(83.25 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 MRTX1133 is a noncovalent, potent, and selective inhibitor targeting KRAS G12D. It occupies the switch II pocket optimally and extends three substituents to facilitate favorable interactions with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 blocks SOS1-catalyzed nucleotide exchange and/or the formation of the KRAS G12D/GTP/RAF1 complex, thereby impeding mutant KRAS-dependent signal transduction. It selectively inhibits KRAS G12D mutant tumor cells while sparing KRAS wild-type cells. MRTX1133 exhibits single-digit nanomolar activity in cellular assays and demonstrates significant efficacy in tumor models with KRAS G12D mutations[1][2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.66mL

0.33mL

0.17mL

8.32mL

1.66mL

0.83mL

16.65mL

3.33mL

1.66mL