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编 号：F506809
分子式：C24H18ClFN4O2
分子量：448.88
分子式：C24H18ClFN4O2
分子量：448.88
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CAS No: 897383-62-9
产品详情
生物活性：
Allitinib (AST-1306) is an orally active and irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively. Allitinib also inhibits ErbB4 with an IC50 of 0.8 nM. Allitinib is an anilino-quinazoline compound and has anti-cancer activity.
体内研究：
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.
体外研究：
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.
Allitinib (AST-1306) is an orally active and irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively. Allitinib also inhibits ErbB4 with an IC50 of 0.8 nM. Allitinib is an anilino-quinazoline compound and has anti-cancer activity.
体内研究：
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.
体外研究：
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.
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