MRTX-EX185

• Description:

  MRTX-EX185 is a potent KRAS (G12D) inhibitor with an IC50 of 90 nM. MRTX-EX185 can binds both GDP-loaded and active GNP states of KRAS and KRAS (G12D) . MRTX-EX185 exhibits broad-spectrum binding properties with IC50s of 110, 290, 130 and 240 nM for KRAS WT, KRAS (G12C), KRAS (Q61H), KRAS (G13D) . MRTX-EX185 also binds GDP-loaded HRAS. MRTX-EX185 can be used to study various RAS-driven tumors (such as pancreatic cancer) [1].

• UNSPSC:

  12352005

• Target:

  Ras

• Type:

  Reference compound

• Related Pathways:

  GPCR/G Protein; MAPK/ERK Pathway

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/mrtx-ex185.html

• Solubility:

  10 mM in DMSO

• Smiles:

  OC1=CC(C2=C(F)C3=NC(OCC45CCCN4CCC5)=NC(N6C[C@@](N7)([H])CC[C@@]7([H])C6)=C3C=N2)=C8C(C#C)=CC=CC8=C1

• Molecular Formula:

  C33H33FN6O2

• Molecular Weight:

  564.65

• References & Citations:

  [1]Vasta JD, et, al. KRAS is vulnerable to reversible switch-II pocket engagement in cells. Nat Chem Biol. 2022 Mar 21.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• Isoform:

  K-Ras

• CAS Number:

  [2621927-57-7]