Allitinib (AST-1306) 是一种具有口服活性且不可逆的EGFR和ErbB2抑制剂，IC50分别为 0.5 和 3 nM。Allitinib 抑制ErbB4，IC50为 0.8 nM。Allitinib 是一种苯胺基喹唑啉化合物，具有抗癌活性。
| 生物活性 | Allitinib (AST-1306) is an orally active and irreversibleEGFRandErbB2inhibitor withIC50s of 0.5 and 3 nM, respectively. Allitinib also inhibitsErbB4with an IC50of 0.8 nM. Allitinib is an anilino-quinazoline compound and has anti-cancer activity[1]. |
| IC50& Target[1] | EGFR 0.5 nM (IC50) | ErbB2 3 nM (IC50) | EGFRL858R/T790M 12 nM (IC50) | ErbB4 0.8 nM (IC50) |
|
体外研究
(In Vitro) | 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[1].
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[1].
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[1].
AST1306 (0.001-1.0 μM; 4 hours) is more than 3000-fold selective for ErbB family kinases over other kinase families[1].
AST1306 potently inhibits the EGFR T790M/L858R double mutant, exhibiting an IC50value of 12 nM[1].
Cell Proliferation Assay[1] | 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[1] | 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. |
|
体内研究
(In Vivo) | 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[1].
| Animal Model: | Nude mice with SK-OV-3 and Calu-3 tumors[1] | | Dosage: | 25, 50, 100 mg/kg | | Administration: | p.o; twice daily; for 28 days | | Result: | Caused a dramatic suppression of tumor growth. |
|
| Clinical Trial | |
| 分子量 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
m.cnreagent.com