MRTX1257

Research use only, not for human use.

MRTX1257 (MRTX-1257, MRTX 1257) is a potent, selective, covalent and irreversible inhibitor of KRAS G12C.

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; demonstrates high selectivity toward the Cys12 of KRAS G12C in NCI-H358 cells, without effect on other free cysteine residues; 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.

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Animal Model:MIA PaCa-2 G12C Xenograft Model (mouse).Dosage:1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg and 100 mg/kg.Administration:Orally daily for 30 days.Result:Showed rapid tumor growth inhibition at all dose groups.Showed sustained regression at 3,10, 30, and 100 mg/kg dose groups.100 mg/kg daily led to complete responses that are maintained >70 days after cessation of treatment.

MRTX-1257 | MRTX 1257

MAPK/ERK Signaling

Ras

Ras

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2206736-04-9

565.722

C33H39N7O2

>98% (HPLC)

In Vitro:?DMSO : 55 mg/mL (97.22 mM)

N#CC[C@@H]1N(C(C=C)=O)CCN(C2=C3C(CN(C4=C5C(C)=CC=CC5=CC=C4)CC3)=NC(OC[C@H]6N(C)CCC6)=N2)C1

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

(-20℃)

With Ice Pack

≥ 2 years