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MRTX1133 is a first-in-class, potent and highly selective KRAS G12D inhibitor. MRTX1133 targets the KRAS G12D protein in both active and inactive states. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 exhibited a long half-life, an ability to bind the KRAS G12D protein in both active and inactive states, and selective inhibition of KRAS G12D mutant cancer cells. In G12D mutant tumor models, MRTX1133 showed dose-dependent selective inhibition of the KRAS pathway and tumor regression.
| Cell Experiment | |
|---|---|
| Cell lines | LS174T cells |
| Preparation method | Briefly, LS174T cells were transfected with lentivirus expressing the CRISPR library that targets the human kinome. The infection was carried out at an MOI of 0.5 with a 500-fold coverage. After puromycin (2 µg/mL) selection for seven days, the surviving cells were harvested. A portion of the cells (equaling a 500-fold coverage of the library) was collected for gDNA extraction (T0), while the remaining cells were plated in 15 cm dishes and cultured in the presence or absence of 25 nM MRTX1133. Cells were refreshed with fresh media or METX1133-containing media every three days and passaged when they were confluent. Ten days after drug treatment, the cells were harvested, and gDNA was extracted using the Blood and Cell Culture DNA Maxi kit according to the manufacturer’s protocols. |
| Concentrations | 25 nM |
| Incubation time | 10 days |
| Animal Experiment | |
|---|---|
| Animal models | Athymic nude mice bearing LS174T xenografts |
| Formulation | 10% DMSO, 40% PEG300, 5% Tween-80, and 45% saline |
| Dosages | 20 mg/kg |
| Administration | i.p. |
| Molecular Weight | 600.63 |
| Formula | C33H31F3N6O2 |
| CAS Number | 2621928-55-8 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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