AST-1306

• CAT Number: I005368
• CAS Number: 897383-62-9
• Molecular Formula: C24H18ClFN4O2
• Molecular Weight: 448.88
• Purity: ≥95%
• Synonyms: N-[4-[3-chloro-4-[(3-fluorophenyl)methoxy]anilino]quinazolin-6-yl]prop-2-enamide
• Target: Protein Tyrosine Kinase/RTK
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: 0.5/3 nM (EGFR/Erb2)[1]
• InChI: 1S/C24H18ClFN4O2/c1-2-23(31)29-17-6-8-21-19(11-17)24(28-14-27-21)30-18-7-9-22(20(25)12-18)32-13-15-4-3-5-16(26)10-15/h2-12,14H,1,13H2,(H,29,31)(H,27,28,30)
• InChIKey: MVZGYPSXNDCANY-UHFFFAOYSA-N
• SMILES: C=CC(=O)NC1=CC2=C(C=C1)N=CN=C2NC3=CC(=C(C=C3)OCC4=CC(=CC=C4)F)Cl

AST-1306 (Cat No.: I005368) is a potent, irreversible inhibitor of epidermal growth factor receptors (EGFR) and human epidermal growth factor receptor 2 (HER2). By covalently binding to these tyrosine kinases, it effectively blocks downstream signaling pathways involved in tumor growth, proliferation, and survival. AST-1306 is being studied for its potential in treating EGFR- and HER2-driven cancers, including non-small cell lung cancer (NSCLC) and breast cancer. Its irreversible binding mechanism offers prolonged inhibition, making it a promising candidate in targeted cancer therapy and drug resistance research.

Reference

[1]. Xie H, Lin L, Tong L et al. AST1306, a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, exhibits antitumor activity both in vitro and in vivo. PLoS One. 2011;6(7):e21487.