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AST-1306 TsOHErbB2 and EGFR inhibitor

AST-1306 TsOH

Catalog No. B1020
Size Price Stock Qty
5mg $165.00 In stock
10mg $265.00 In stock
50mg $880.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

AST-1306 TsOH

Biological Activity

Description AST-1306 TsOH is a selective and irreversible inhibitor of ErbB2 and EGFR with IC50 values of 0.5 nM and 3 nM, respectively.
Targets ErbB2 EGFR        
IC50 0.5 nM 3 nM        

AST-1306 TsOH Dilution Calculator

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Chemical Properties

Cas No. 1050500-29-2 SDF Download SDF
Chemical Name N-[4-[3-chloro-4-[(3-fluorophenyl)methoxy]anilino]quinazolin-6-yl]prop-2-enamide;4-methylbenzenesulfonic acid
Canonical 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
Formula C31H26ClFN4O5S M.Wt 621.08
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips N/A
Shipping Condition N/A

Background

AST-1306 is a selective, irreversible inhibitor of ErbB2 and EGFR with IC50 values of 0.5nM and 3nM, respectively [1].

AST-1306 is designed and synthesized based on the chemical structure of lapatinib. The molecular docking method shows AST-1306 binds to the ATP-binding pocket of the kinases and form covalent bind with certain amino acids. AST-1306 can inhibit EGFR and ErbB2 in a cell-free assay with more than 3000-fold selectivity to other kinases. Besides the wild-type EGFR, AST-1306 also inhibits EGFR mutant T790M/L858R both in a cell-free assay and in HIH3T3 cells. The growth of the cells is suppressed by AST-1306 due to the inhibition of the phosphorylation of EGFR. It also occurs in some human cancer cells. Experiments have proved that AST-1306 notly inhibits the phosphorylation of EGFR and ErbB2 and subsequently decreases the downstream pathways of these kinases in A549 cells, Calu-3 cells and SK-OV-3 cells. Moreover, AST-1306 potently inhibits the tumor growth both in ErbB2-overexpressing xenograft models and FVB-2/Nneu transgenic mouse model [1].

References:
[1] Xie H, Lin L, Tong L, Jiang Y, Zheng M, Chen Z, Jiang X, Zhang X, Ren X, Qu W, Yang Y, Wan H, Chen Y, Zuo J, Jiang H, Geng M, Ding J. 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.