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MRTX1133

58 Cited Publications
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Based on 58 publication(s) in Google Scholar

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.

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  • 純度: 99.97%
  • CAS 番号: 2621928-55-8
  • 分子式: C33H31F3N6O2
  • 分子量:600.63
  • 保管条件:
    Powder   -20°C, 3 years , 4°C, 2 years ; In solvent   -80°C, 6 months , -20°C, 1 month
  • MRTX1133 Chemical Structure
    MRTX1133 構造式
  • Experimental Validation Results for MRTX1133
  • Experimental Validation Results for MRTX1133
  • Experimental Validation Results for MRTX1133
  • Experimental Validation Results for MRTX1133
  • Experimental Validation Results for MRTX1133
CAS 番号: 2621928-55-8
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  • MRTX1133 Chemical Structure
    MRTX1133 Chemical Structure
    1/16
  • 1/16

    MRTX1133 purchased from MedChemExpress. Usage Cited in: Nature. 2026 Jan;649(8098):1022-1031. [Abstract]

    Customer Validation
     MRTX1133 (10, 100 nM; 24 h). KPC cells were treated for 24 h and analysed using quantitative PCR with reverse transcription (RT–qPCR)

  • 1/16

    MRTX1133 purchased from MedChemExpress. Usage Cited in: Nature. 2026 Jan;649(8098):1022-1031. [Abstract]

    Customer Validation
     MRTX1133 (1, 10, 100 nM; 24 h) was used to treat KPC cells for 24 h, and the cells were analysed using immunoblotting.

  • 1/16

    MRTX1133 purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2024 Oct 4;14(10):1964-1989. [Abstract]

    Customer Validation
     MRTX1133 (0.5 μM; 24 h)-treated 9805 cells produce conditioned medium (CM) that induces a reduction in Il33 expression in CD1WT fibroblasts.

  • 1/16

    MRTX1133 purchased from MedChemExpress. Usage Cited in: Cancer Res. 2024 Nov 4;84(21):3629-3639. [Abstract]

    Customer Validation
     PDAC cell lines grown in low confluent collagen cultures were treated with MRTX1133 (0.5 μmol/L) for 8 hours, and the effect on ERK1/2 phosphorylation was analyzed by Western blotting.

  • 1/16

    MRTX1133 purchased from MedChemExpress. Usage Cited in: Immunity. 2023 Nov 14;56(11):2570-2583.e6. [Abstract]

    Customer Validation
     Western blot showing phosphorylated and total ERK1/2 in lysates of KRASG12D-mutated A427 cells, treated with anti-KRASG12D-IgA1 or MRTX1133.

  • MRTX1133