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AST-1306 TsOH CAS: 1050500-29-2

Category: Inhibitors
Product Name: AST-1306 TsOH
Cat No: I000278
CAS No: 1050500-29-2
Synonyms: N-[4-[3-chloro-4-[(3-fluorophenyl)methoxy]anilino]quinazolin-6-yl]prop-2-enamide;4-methylbenzenesulfonic acid
Molecular Formula: C31H26ClFN4O5S
Molecular Weight: 621.08
SMILES: CC1=CC=C(C=C1)S(=O)(=O)O.C=CC(=O)NC1=CC2=C(C=C1)N=CN=C2NC3=CC(=C(C=C3)OCC4=CC(=CC=C4)F)Cl
Solubility: in DMSO > 10 mM
Target: EGFR
IC50: 0.5/3 nM (EGFR/Erb2)[1]
Storage: powder
CAS 1050500-29-2,AST-1306 TsOH
  • Description

AST-1306 TsOH 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/L858R
AST-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.

  • References


[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.


price inquiry for CAS:1050500-29-2, Product:AST-1306 TsOH