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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