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MRTX-1257

Product Specifications

CAS Number

2206736-04-9

Target

Ras, Kras

Related Pathways

GPCR/G Protein, MAPK

Purity

0.9907

Bioactivity

MRTX-1257 is a selective, irreversible, and covalent inhibitor of KRAS G12C with an IC50 of 900 pM for KRAS-dependent ERK phosphorylation in H358 cells. MRTX-1257 demonstrated 31% bioavailability in the mouse, with free fraction exposures well above cellular potency, and 77% target engagement in a PK/PD experiment.

Smiles

CN1CCC[C@H]1COc1nc2CN(CCc2c(n1)N1CCN([C@@H](CC#N)C1)C(=O)C=C)c1cccc2cccc(C)c12

Molecular Formula

C33H39N7O2

Molecular Weight

565.71

Shipping Conditions

Ice Packs

Storage Temperature

-20°C

Available Sizes

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