Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MRTX-1257 is a selective, irreversible, and covalent inhibitor of KRAS G12C. It has an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells. MRTX1257 demonstrated 31% bioavailability in the mouse, with free fraction exposures well above the cellular potency In a PK/PD experiment, 77% target engagement.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 58.00 | |
2 mg | In stock | $ 82.00 | |
5 mg | In stock | $ 133.00 | |
10 mg | In stock | $ 231.00 | |
25 mg | In stock | $ 391.00 | |
50 mg | In stock | $ 586.00 | |
100 mg | In stock | $ 838.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 179.00 |
Description | MRTX-1257 is a selective, irreversible, and covalent inhibitor of KRAS G12C. It has an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells. MRTX1257 demonstrated 31% bioavailability in the mouse, with free fraction exposures well above the cellular potency In a PK/PD experiment, 77% target engagement. |
In vivo | MRTX-1257 shows sustained regression at 3,10, 30, and 100 mg/kg dose groups. MRTX-1257 dosed of 100 mg/kg daily causes complete responses that are maintained >70 days after cessation of treatment. MRTX-1257 (1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg and 100 mg/kg, orally, daily for 30 days) displays rapid tumor growth inhibition at all dose groups in MIA PaCa-2 G12C Xenograft model in mice . |
Molecular Weight | 565.71 |
Formula | C33H39N7O2 |
CAS No. | 2206736-04-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 54 mg/mL(95.46 mM)
You can also refer to dose conversion for different animals. More
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MRTX-1257 2206736-04-9 GPCR/G Protein MAPK Ras Inhibitor selective inhibit G12C irreversible ERK phosphorylation H358 cells cancer mutant MRTX1257 covalent MRTX 1257 KRAS inhibitor