MRTX1257

Modify Date: 2024-01-12 09:51:26

MRTX1257 Structure
MRTX1257 structure
Common Name MRTX1257
CAS Number 2206736-04-9 Molecular Weight 565.71
Density N/A Boiling Point N/A
Molecular Formula C33H39N7O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of MRTX1257


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].

 Names

Name MRTX-1257

 MRTX1257 Biological Activity

Description 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].
Related Catalog
Target

IC50: 900 pM (KRAS dependent ERK phosphorylation in H358 cells)[1].

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

[1]. Matthew et al. Structure-Based Drug Discovery of MRTX1257, a Selective, Covalent KRAS G12C Inhibitor with Oral Activity in Animal Models of Cancer.

 Chemical & Physical Properties

Molecular Formula C33H39N7O2
Molecular Weight 565.71
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