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Chemical Structure : MRTX1257
CAS No.: 2206736-04-9
Catalog No.: PC-35952Not For Human Use, Lab Use Only.
MRTX1257 (MRTX-1257, MRTX 1257) is a potent, selective, covalent and irreversible inhibitor of KRAS G12C, inhibits KRAS dependent ERK-phosphorylation in the H358 cell with IC50 of 0.9 nM.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $128 | In stock | |
| 10 mg | $198 | In stock | |
| 25 mg | $348 | In stock | |
| 50 mg | $548 | In stock | |
| 100 mg | Get quote |
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MRTX1257 (MRTX-1257, MRTX 1257) is a potent, selective, covalent and irreversible inhibitor of KRAS G12C, inhibits KRAS dependent ERK-phosphorylation in the H358 cell with IC50 of 0.9 nM.
MRTX1257 demonstrates high selectivity toward the Cys12 of KRAS G12C in NCI-H358 cells, without effect on other free cysteine residues.
MRTX1257 shows sustained regression at 3,10, 30, and 100 mg/kg dose in MIA PaCa-2 xenografts, shows rapid growth inhibition and durable efficacy even after dosing was stopped, and MRTX1257 is orally acitve.
| M.Wt | 565.722 | |
| Formula | C33H39N7O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
2-((S)-1-acryloyl-4-(7-(8-methylnaphthalen-1-yl)-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)piperazin-2-yl)acetonitrile |
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1. U.S. Pat. Appl. Publ. (2018), US 20180072723 A1 20180315.
2. Khan HY, et al. Cancer Res Commun. 2022 May;2(5):342-352.
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