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AST-1306EGFR/HER2 inhibitor

AST-1306

Catalog No. A8367
Size Price Stock Qty
5mg $176.00 In stock
10mg $308.00 In stock
50mg $836.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

AST-1306

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Chemical Properties

Cas No. 897383-62-9 SDF Download SDF
Synonyms AST1306; AST 1306
Chemical Name N-[4-[3-chloro-4-[(3-fluorophenyl)methoxy]anilino]quinazolin-6-yl]prop-2-enamide
Canonical SMILES C=CC(=O)NC1=CC2=C(C=C1)N=CN=C2NC3=CC(=C(C=C3)OCC4=CC(=CC=C4)F)Cl
Formula C24H18ClFN4O2 M.Wt 448.88
Solubility >22.5mg/mL in DMSO Storage Store at -20°C
General tips N/A
Shipping Condition N/A

Background

AST1306 is a novel inhibitor of EGFR and HER2 (IC50 = 0.5 nM and 3 nM respectively)

EGFR (epidermal growth factor receptor) is a cell-surface receptor tyrosine kinase. The receptor activation leads to dimerization and tyrosine autophosphorylation. It induces a cascade of downstream cellular responses such as modification in gene expression, cell proliferation and cytoskeletal rearrangement etc. HER2 is a member of the epidermal growth factor and is associated with breast and ovarian cancers.

AST1306 selectively blocked EGFR and HER2 kinase activities in a cell-free assay. The tyrosine kinase activity of EGFR mutant T790M/L858R was also inhibited by AST1306 in intact cell and cell-free assays. In addition, AST1306 attenuated the EGFR and HER2 phosphorylation and downstream substrates. [1]

In ErbB2-overexpressing xenograft and FVB-2/Nneu transgenic mouse model, AST1306 potently inhibited tumor growth. In SK-OV-3 xenograft model, AST1306 caused a quick and long-lasting (≥24h) inhibition of EGFR and HER2. [1]

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.