AZD0022

SKU: orb2945999

Description

AZD0022 is a selective, reversible, and orally active KRAS G12D inhibitor with high affinity for both GTP- and GDP-bound states, while sparing wild-type KRAS. It demonstrates anti-tumor activity in preclinical models of pancreatic ductal adenocarcinoma (PDAC) and non-small cell lung cancer (NSCLC), supporting its investigation for advanced solid tumors.

Research Area

Signal Transduction

Key Properties

• CAS Number: 2958627-18-2
• MW: 614.64
• Purity: 98.73% (May vary between batches)
• Formula: C₃₄H₃₀F₄N₆O
• SMILES: FC=1C=CC2=CC(N)=CC(C=3C(F)=CC=4C(=NC(=NC4N5CC6C=CC(N6)C5)OCC78N(CCC7)CC(F)C8)C3F)=C2C1C#C
• Target: Ras
• Solubility: 10% DMSO+40% PEG300+5% Tween-80+45% Saline:3.3 mg/mL (5.37 mM);DMSO:80 mg/mL (130.16 mM)

Bioactivity

• In Vivo:
  In nude mice bearing GP2D human tumor xenografts, oral dosing of AZD0022 at 150 mg/kg led to sustained plasma and tumor exposure, with tumor concentrations approximately 18-fold higher than plasma. Seven days of BID dosing at 150 mg/kg resulted in up to 75% inhibition of pRSK, with dose-dependent target modulation observed across 10, 50, and 150 mg/kg.
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• In Vitro:
  PKPD modelling of AZD0022 suggested an unbound IC50 of 1.4 nM for pRSK inhibition.

Storage & Handling

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

Alternative Names

AZD 0022

Compound Identifiers

PubChem CID

176455489