MRTX-1257

• 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:

  Cool pack

• Storage Temperature:

  -20°C

• CAS Number:

  2206736-04-9