AZ5104

SKU: orb1226315

Description

AZ5104, the demethylated metabolite of AZD-9291, is a potent EGFR inhibitor with IC50 of <1 nM, 6 nM, 1 nM, and 25 nM for EGFR (L858R/T790M), EGFR (L858R), EGFR (L861Q), and EGFR (wildtype), respectively. Phase 1.

Key Properties

• CAS Number: 1421373-98-9
• MW: 485.58
• Purity: >98% (HPLC)
• Formula: C₂₇H₃₁N₇O₂
• SMILES: C=CC(NC1=CC(NC2=NC=CC(C3=CNC4=C3C=CC=C4)=N2)=C(OC)C=C1N(CCN(C)C)C)=O.
• Target: EGFR
• Solubility: Ethanol: 23 mg/mL warmed (47.36 mM); DMSO: 97 mg/mL (199.76 mM)

Bioactivity

• In Vivo:
  The metabolite, AZ5104 (5 mg/kg/day), is effective in shrinking tumors in both C/L858R and C/L+T mice.
• In Vitro:
  AZ-5104 inhibits EGFR phosphorylation with IC50s of 2, 1, 2, 53, and 33 nM in H1975 (EGFRL858R/T790M), PC-9VanR (EGFRExon 19 deletion/T790M), PC-9 (EGFRExon 19 deletion), H2073 (WT), and LOVO (WT), respectively. AZ5104 exhibits a reduced selectivity margin against wild-type EGFR when compared to AZD9291. AZ5104 display minimal off-target activity against other non-HER family kinases, but has the potential to target both HER2 and HER4 kinase activity.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AZ5104 | AZ-5104 | AZ 5104. Demethylated AZ9291. metabolite of AZD9291

Quick Database Links

Gene Symbol

EGFR