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MRTX1133

T9303
TargetMol Chemicals
CAS Number2621928-55-8
Product group Chemicals
Molecular Weight600.63
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Overview

  • Supplier
    TargetMol Chemicals
  • Product Name
    MRTX1133
  • Delivery Days Customer
    4
  • CAS Number
    2621928-55-8
  • Category Supplier
    Chemical
  • Chemical Name
    MRTX1133
  • Molecular Formula
    C33H31F3N6O2
  • Molecular Weight
    600.63
  • Scientific Description
    MRTX1133 is a potent, selective, and noncovalent inhibitor of KRAS G12D. MRTX1133 exhibits an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 inhibits mutant KRAS-dependent signal transduction by preventing SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex. MRTX1133 selectively inhibits KRAS G12D mutant tumor cells with no effect on KRAS wild-type. MRTX1133 exhibits single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations.
  • Shelf life instruction
    3 years
  • SMILES
    C(OC=1N=C(C2=C(N1)C(F)=C(N=C2)C=3C4=C(C=C(O)C3)C=CC(F)=C4C#C)N5CC6NC(C5)CC6)[C@@]78N(C[C@H](F)C7)CCC8
  • Storage Instruction
    -20°
  • UNSPSC
    12352200

References

  • Xiaolun Wang, et al.Identification of MRTX1133, a Noncovalent, Potent, and Selective KRAS G12D Inhibitor.J Med Chem . 2021 Dec 10. doi: 10.1021/acs.jmedchem.1c01688.