Allitinib,897383-62-9

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Allitinib

CAS No. : 897383-62-9

MCE 国际站：Allitinib

产品活性：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。

研究领域：Protein Tyrosine Kinase/RTK | JAK/STAT Signaling

作用靶点：EGFR

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.
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.

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.

相关产品：Gefitinib | Osimertinib | Erlotinib | Afatinib | Trastuzumab | AG-490 | Cetuximab | Lapatinib | Neratinib | Genistein | Dacomitinib | AG-1478 | Poziotinib | Tucatinib | Sapitinib | TAS6417 | Pyrotinib | Mubritinib | BI-4020 | Icotinib | Pertuzumab | AZ-5104 | AZD3759 | BMS-690514 | CUDC-101

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