MRTX1133
Catalogue number:
HY-134813-10mg
Supplier:
Size:
10 mg
Product is available in:
This product is for research use only and is not for human consumption or therapeutic use.
CAS Number:
2621928-55-8
Purity:
99.97
Molecular Formula:
C33H31F3N6O2
Molecular Weight:
600.63
Mass Spectrometry:
Reference Materials
- Data sheet: View or download
- MSDS: View or download
- Protocol: View or download
Product Description:
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 KD 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[1][2].