Biological Activity
MRTX-1257 is a selective, irreversible, covalent and oral active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells[1].
In Vitro
No in vitro data are provided in the current product source. Contact us for further information.
In Vivo
MRTX-1257 (1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg and 100 mg/kg, orally, daily for 30 days) shows rapid tumor growth inhibition at all dose groups in MIA PaCa-2 G12C Xenograft model in mice[1]. MRTX-1257 shows sustained regression at 3,10, 30, and 100 mg/kg dose groups[1]. MRTX-1257 dosed of 100 mg/kg daily leads to complete responses that are maintained >70 days after cessation of treatment[1]. Animal Model: MIA PaCa-2 G12C Xenograft Model (mouse)[1]. Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg and 100 mg/kg. Administration: Orally daily for 30 days. Result: Showed rapid tumor growth inhibition at all dose groups. Showed sustained regression at 3,10, 30, and 100 mg/kg dose groups. 100 mg/kg daily led to complete responses that are maintained >70 days after cessation of treatment.
References & source
[1]. Matthew et al. Structure-Based Drug Discovery of MRTX1257, a Selective, Covalent KRAS G12C Inhibitor with Oral Activity in Animal Models of Cancer.
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.