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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]. |
Animal study | MRTX1133 demonstrates efficacy in a xenograft mouse tumor model harboring the KRAS G12D mutation[1]. |
计算器 | ||||
存储液制备 | ![]() |
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 |
CAS号 | 2621928-55-8 |
分子式 | C33H31F3N6O2 |
分子量 | 600.63 |
SMILES Code | C(OC=1N=C(C2=C(N1)C(F)=C(N=C2)C=3C4=C(C=C(O)C3)C=CC(F)=C4C#C)N5CC6NC(C5)CC6)[C@@]78N(C[C@H](F)C7)CCC8 |
MDL No. | MFCD34567005 |
别名 | |
运输 | 蓝冰 |
InChI Key | SCLLZBIBSFTLIN-IFMUVJFISA-N |
Pubchem ID | 156124857 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place, sealed in dry, 2-8°C |