Allitinib

SKU: orb1308633

Description

Allitinib (AST-1306) is an irreversible, potent inhibitor of EGFR and ErbB2, exhibiting IC50 values of 0.5 nM and 3 nM, respectively. This small molecule is utilized in cancer research, demonstrating antitumor efficacy in both cellular assays and in vivo models of various carcinomas.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 897383-62-9
• MW: 448.88
• Purity: 99.10%
• Formula: C₂₄H₁₈ClFN₄O₂
• SMILES: N(C=1C2=C(C=CC(NC(C=C)=O)=C2)N=CN1)C3=CC(Cl)=C(OCC4=CC(F)=CC=C4)C=C3
• Target: EGFR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.46 mM);DMSO:55 mg/mL (122.53 mM)

Bioactivity

• Target IC50:
  EGFR:0.5 nM|EGFR (L858R/T790M):12 nM|ErbB2:3 nM|ERB4:0.8 nM
• In Vivo:
  AST1306 (AST-1306; oral; 25-100 mg/kg) significantly inhibited tumor growth in SK-OV-3 and Calu-3 xenograft models.
• In Vitro:
  AST1306 (AST-1306; 0.19-6.25 μM; 72 hours) inhibits the growth of HIH3T3-EGFR T790M/L858R cells. AST1306 (0.001-1.0 μM; 4 hours) is more than 3000-fold selective for ErbB family kinases over other kinase families. In A549, Calu-3, and SK-OV-3 cells, AST1306 inhibits tyrosine kinase activation and downstream signaling pathways, and dose-dependently and markedly inhibits EGF-induced EGFR phosphorylation in A549 cells.

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

HER1, Epidermal growth factor receptor, EGFRL858R/T790M, EGFR (T790M/L858R), EGFR, ErbB4, ErbB2, ErbB-1, Irreversible, inhibit, Inhibitor, ALS1306, ALS-1306, Allitinib, anti-cancer, ALS 1306, anilino-quinazoline, AST 1306, AST1306, AST-1306

Compound Identifiers

PubChem CID

24739943