KRAS G12C inhibitor 11( —— )

Catalog No. M13445 CAS No. 2158297-63-1

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Product Name

KRAS G12C inhibitor 11
Note

Research use only, not for human use.
Brief Description

KRAS G12C inhibitor 11 is a potent, selective, covalent and irreversible inhibitor of KRAS G12C.
Description

KRAS G12C inhibitor 11 is a potent, selective, covalent and irreversible inhibitor of KRAS G12C, inhibits KRAS dependent ERK-phosphorylation in the H358 cell with IC50 of 5 nM; demonstrates super proportional dose ascending oral exposure in mice with 3h target coverage at the 30 mg/kg dose; shows rapid growth inhibition and durable efficacy even after dosing was stopped, orally active.
In Vitro

Kirsten Rat Sarcoma 2 Viral Oncogene Homolog (KRas) is a small GTPase and a member of the Ras family of oncogenes. KRas serves a molecular switch cycling between inactive (GDP -bound) and active (GTP -bound) states to transduce upstream cellular signals received from multiple tyrosine kinases to downstream effectors to regulate a wide variety of processes, including cellular proliferation.
In Vivo

——
Synonyms

——
Pathway

MAPK/ERK Signaling
Target

Ras
Recptor

Ras
Research Area

——
Indication

——

CAS Number

2158297-63-1
Formula Weight

551.695
Molecular Formula

C32H37N7O2
Purity

>98% (HPLC)
Solubility

——
SMILES

CN1CCCC1COC2=NC3=C(CCN(C3)C4=CC=CC5=CC=CC=C54)C(=N2)N6CCN(C(C6)CC#N)C(=O)C=C
Chemical Name

2-((S)-1-acryloyl-4-(2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-7-(naphthalen-1-yl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)piperazin-2-yl)acetonitrile

1. U.S. Pat. Appl. Publ. (2018), US 20180072723 A1 20180315.

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