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]

AST-1306 is a novel irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, also effective in mutation EGFR T790M/L858R, more potent to ErbB2-overexpressing cells, 3000-fold selective for ErbB family than other kinases.IC50 value: 0.5/3 nM (EGFR/Erb2)[1]Target: EGFR/Erb2;Mutant EGFR T790M/L858RAST-1306 functions as an irreversible inhibitor, most likely through covalent interaction with Cys797 and Cys805 in the catalytic domains of EGFR and ErbB2, respectively. Further studies showed that AST-1306 inactivated pathways downstream of these receptors and thereby inhibited the proliferation of a panel of cancer cell lines. AST-1306 is a potent(pM) and selective inhibitor of EGFR and ErbB4 (IC50 = 500pM and 800 pM, respectively). AST-1306 blocks phosphorylation of EGFR and also prevents downstream pathways. AST-1306 also dose-dependently inhibits EGF-induced EGFR phosphorylation in the A549 cancer cell line.

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.