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KRAS G12C inhibitor 11

Chemical Structure : KRAS G12C inhibitor 11

CAS No.: 2158297-63-1

KRAS G12C inhibitor 11

Catalog No.: PC-35953Not For Human Use, Lab Use Only.

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.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 551.695
Formula C32H37N7O2
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-(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

References

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

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