Allitinib tosylateAllitinib tosylate
MedChemExpress (MCE)
HY-13427
1050500-29-2
AST-1306 (TsOH)
99.83%
4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months
-20°C, 1 month (sealed storage, away from moisture)
Room temperature in continental US
may vary elsewhere.
Allitinib tosylate (AST-1306 (TsOH)) is an orally active and irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively. Allitinib tosylate also inhibits ErbB4 with an IC50 of 0.8 nM. Allitinib tosylate is an anilino-quinazoline compound and has anti-cancer activity
AST1306 tosylate (AST-1306 (TsOH)
0.19-6.25 μM
72 hours) induces a significant, concentration-dependent inhibition of the growth of HIH3T3-EGFR T790M/L858R cells[1]. AST1306 tosylate inhibits the activation of tyrosine kinases and downstream signaling pathways in A549 cells, Calu-3 cells and SK-OV-3 cells. AST1306 tosylate dose-dependently and markedly inhibits EGF-induced EGFR phosphorylation in A549 cells[1]. AST1306 tosylate (0.1, 0.5, 1.0, 5.0 μM) can dramatically inhibit the growth of both tumor cells on soft agar, and SK-OV-3 cells exhibited much more sensitivity than that of A549 cells[1]. AST1306 tosylate (0.001-1.0 μM
4 hours) is more than 3000-fold selective for ErbB family kinases over other kinase families[1]. AST1306 tosylate potently inhibits the EGFR T790M/L858R double mutant, exhibiting an IC50 value of 12±2 nmol/L[1].
AST1306 tosylate (AST-1306 (TsOH)
p.o.
25-100 mg/kg
twice daily
for 28 days) causes a dramatic suppression of tumor growth in SK-OV-3 and Calu-3 xenograft models[1].
EGFR 0.5 nM (IC50) ErbB2 3 nM (IC50) EGFRL858R/T790M 12 nM (IC50) ErbB4 0.8 nM (IC50)
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[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. [Content Brief]