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MRTX1257

Chemical Structure : MRTX1257

CAS No.: 2206736-04-9

MRTX1257 (MRTX-1257, MRTX 1257)

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.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 565.722
Formula C33H39N7O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

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

References

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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