Divarasib

SKU: orb1737448

Description

Divarasib (GDC-6036) is a potent, selective, and oral KRAS G12C inhibitor with sub-nanomolar IC50, which irreversibly traps the oncoprotein in an inactive state to suppress tumor growth. It is actively researched in vitro and in vivo for treating solid tumors such as non-small cell lung cancer and colorectal cancer.

Research Area

Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 2417987-45-0
• MW: 622.06
• Purity: 99.96% (May vary between batches)
• Formula: C₂₉H₃₂ClF₄N₇O₂
• SMILES: C[C@H]1CN(CCN1c1nc(OC[C@@H]2CCCN2C)nc2c(F)c(c(Cl)cc12)-c1nc(N)cc(C)c1C(F)(F)F)C(=O)C=C
• Target: Ras,Kras
• Solubility: 10% DMSO+40% PEG300+5% Tween-80+45% Saline:3.3 mg/mL (5.3 mM);DMSO:90 mg/mL (144.68 mM)

Bioactivity

• Target IC50:
  HCC1171 cells:2 nM (EC50)|KRas (G12C):< 0.01 μM
• In Vivo:
  Administration of Divarasib (10-100 mg/kg/day; PO for 7 days) results in a reduction in the ratio of free KRAS G12C.
• In Vitro:
  Divarasib exhibits a potency with an EC50 value of 2 nM in K-Ras G12C-alkylation HCC1171 cells.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Divarasib, KRAS G12C, GDC6036, GDC-6036, GDC 6036

Compound Identifiers

PubChem CID

146624881