Copy Link Print Information

MRTX1133

58 Cited Publications
Revisión del cliente

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.

Para uso exclusivo en investigación. No vendemos a pacientes.

  • Pureza: 99.97%
  • No. CAS: 2621928-55-8
  • Fòrmula: C33H31F3N6O2
  • Peso molecular:600.63
  • Almacenamiento:
    Powder   -20°C, 3 years , 4°C, 2 years ; In solvent   -80°C, 6 months , -20°C, 1 month
  • MRTX1133 Chemical Structure
    MRTX1133 Chemical Structure
  • 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
No. CAS: 2621928-55-8
Tamaño
Precio
Stock
Cantidad
Amount: USD 0.00
Please select quantity
or
or

* Seleccione Cantidad antes de agregar artículos.

To place orders, for customer services and technical support, please contact: MedChemExpress USA

Tel: 609-228-6898 E-mail: [email protected] [email protected]

Data Download
Other Forms of MRTX1133:

To place orders, for customer services and technical support, please contact:

609-228-6898
[email protected] [email protected]
Encuentre su distribuidor local Your local distributor: Hycultec GmbHHycultec
  • Actividad biológica
  • Chemical Information
  • Solvente y solubilidad
  • Pureza y Documentación
  • Referencias
  • Help & FAQs
You May Still Need
Top Publications Citing

Use of MCE Products

Publications Citing Use of MedChemExpress (MCE) MRTX1133

More
Customer Validation & Images
RT-PCRWB
  • RT-PCR
  • WB
  • RT-PCR
  • WB
  • WB

Ver todos los productos específicos de isoformas Ras

More
Keywords
MOQ
Minimum order quantity
100 mg

Obtener un presupuesto En stock

Other size
Obtener un presupuesto
Please select quantity
Amount: USD 0.00
Sign in to MedChemExpress Inicie sesiòn
Registrar
Sign in to MedChemExpress
Registrar una cuenta nueva

At least 6 characters

Personalize your experience, you are currently not signed in. For a better experience, please create an online profile, you can:

Obtain points redemption prizes
Check out faster
Add multiple shipping locations
View orders
Assay Types
  • 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