AZ-5104

SKU: orb1305403

Description

AZ5104 is a selective and potent small molecule inhibitor of the epidermal growth factor receptor (EGFR). It is widely used in biochemical and cellular assays to study EGFR-driven signaling pathways and has demonstrated research utility in both in vitro and in vivo models of oncology.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1421373-98-9
• MW: 485.58
• Purity: 99.90% (May vary between batches)
• Formula: C₂₇H₃₁N₇O₂
• SMILES: COc1cc(N(C)CCN(C)C)c(NC(=O)C=C)cc1Nc1nccc(n1)-c1c[nH]c2ccccc12
• Target: EGFR
• Solubility: Ethanol:16 mg/mL (32.95 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.8 mM);DMSO:90 mg/mL (185.35 mM)

Bioactivity

• Target IC50:
  EGFR (L861Q):1 nM|EGFR (WT):25 nM|EGFR (L858R):6 nM|ERB4:7 nM|EGFR (L858R/T790M):<1 nM
• In Vivo:
  In both C/L858R and C/L+T mice, AZ5104 (5 mg/kg/d, p.o.) induces significant and sustained tumor regression.
• In Vitro:
  AZ5104 shows great potency against ex19del (2 nM in PC-9), T790M (2 nM in H1975), and wild-type EGFR (33 nM in LOVO) cell lines. AZ5104 causes inhibition of cell viability with IC50 of 3.3 nM, 2.6 nM, 80 nM, and 53 nM for H1975 (T790M/L858R), PC-9 (ex19del), Calu 3 (WT), and NCI-H2073 (WT), respectively.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, HER1, HER2/ErbB2, EGFR, EGFR (L858R), EGFR (L861Q), EGFR (L858R/T790M), EGFR (wildtype), Epidermal growth factor receptor, ErbB-1, AZ5104, AZ-5104, AZ 5104

Compound Identifiers

PubChem CID

71496460