MRTX1133

Overview

MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated K D against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations.

Application

Products | Products > Signaling Pathways > GPCR/G Protein | Products > Signaling Pathways > MAPK/ERK Pathway | Products > Research Areas > Cancer | Products > Research Areas > Cancer > Cancer Targeted Therapy | Products > Research Areas > Cancer > Cancer Metabolism and Metastasis | Products > Signaling Pathways > Ras

Product Information

• Catalog No.: HY-134813
• CAS No.: 2621928-55-8
• Molecular Formula: C33H31F3N6O2
• Molecular Weight: 600.63
• Purity: 99.97%
• Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
• Solubility: 3.5 mg/mL (5.83 mM); Suspended solution; Need ultrasonic
• Availability: In-stock

Source

Original product source