Allitinib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Allitinib (AST-1306) 具有抗癌活性，是不可逆的 EGFR 和 ErbB2 抑制剂，IC50 分别为 0.5 和 3 nM。

Allitinib (AST-1306) has anti-cancer activity，and it is an irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively. (In Vitro):AST1306 (AST-1306; 0.19-6.25 μM; 72 hours) inhibit the growth of HIH3T3-EGFR T790M/L858R cells. AST1306 (0.001-1.0 μM; 4 hours) is more than 3000-fold selective for ErbB family kinases over other kinase families. AST1306 inhibits the activation of tyrosine kinases and downstream signaling pathways in A549 cells, Calu-3 cells and SK-OV-3 cells，and dose-dependently and markedly inhibits EGF-induced EGFR phosphorylation in A549 cells.(In Vivo):AST1306 (AST-1306; oral; 25-100 mg/kg) significantly inhibited tumor growth in SK-OV-3 and Calu-3 xenograft models.

AST1306 (AST-1306; 0.19-6.25 μM; 72 hours) induces a significant, concentration-dependent inhibition of the growth of HIH3T3-EGFR T790M/L858R cells. AST1306 inhibits the activation of tyrosine kinases and downstream signaling pathways in A549 cells, Calu-3 cells and SK-OV-3 cells. AST1306 dose-dependently and markedly inhibits EGF-induced EGFR phosphorylation in A549 cells. AST1306 (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. AST1306 (0.001-1.0 μM; 4 hours) is more than 3000-fold selective for ErbB family kinases over other kinase families. AST1306 potently inhibits the EGFR T790M/L858R double mutant, exhibiting an IC50 value of 12 nM. Cell Proliferation Assay Cell Line:NIH3T3 parental cells and NIH3T3 cells Concentration:0.19, 0.39, 0.78, 1.56, 3.13, 6.25 μM Incubation Time:72 hours Result:Induced a significant, concentration-dependent inhibition of the growth of HIH3T3-EGFR T790M/L858R cells.Western Blot Analysis Cell Line:A549 cells , Calu-3 cells and SK-OV-3 cells Concentration:0.001, 0.01, 0.1, 1.0 μM Incubation Time:4 hours Result:Inhibits the activation of tyrosine kinases and downstream signaling pathways.

AST1306 (AST-1306; 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. Animal Model:Nude mice with SK-OV-3 and Calu-3 tumors Dosage:25, 50, 100 mg/kg Administration:p.o; twice daily; for 28 days Result:Caused a dramatic suppression of tumor growth.

AST-1306 | ALS 1306

Angiogenesis

EGFR

A1

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897383-62-9

448.88

C24H18ClFN4O2

>98% (HPLC)

——

Fc1cccc(COc2ccc(Nc3ncnc4ccc(NC(=O)C=C)cc34)cc2Cl)c1

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(-20℃)

With Ice Pack

≥ 2 years