MRTX1133 (formic)

• Description:

  MRTX1133 formic is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 formic 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 formic prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRASG12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 formic shows efficacy in tumor models harboring KRAS G12D mutations[1][2].

• UNSPSC:

  12352005

• Target:

  Ras

• Related Pathways:

  GPCR/G Protein; MAPK/ERK Pathway

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Purity:

  98.23

• Solubility:

  DMSO : 50 mg/mL (ultrasonic) |H2O : 25 mg/mL (ultrasonic; warming; heat to 60°C)

• Smiles:

  O=CO.OC1=CC(C2=C(F)C3=NC(OC[C@]45C[C@@H](F)CN4CCC5)=NC(N6C[C@H]7N[C@H](CC7)C6)=C3C=N2)=C8C(C#C)=C(F)C=CC8=C1

• Molecular Formula:

  C34H33F3N6O4

• Molecular Weight:

  646.66

• References & Citations:

  [1]KRAS G12D Inhibitor: MRTX1133. [ (accessed on 22 April 2021) ];2021 Available online.|[2]Wang X, et al. Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor [published online ahead of print, 2021 Dec 10]. J Med Chem. 2021;10.1021/acs.jmedchem.1c01688.|[3]KRAS G12D Inhibitor: MRTX1133. [ (accessed on 22 April 2021) ];2021 Available online.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  4°C (Powder, sealed storage, away from moisture)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Phase 1

• Isoform:

  K-Ras