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Ceritinib dihydrochloride

CAS No. : 1380575-43-8

MCE 站：Ceritinib dihydrochloride

产品活性：Ceritinib dihydrochloride (LDK378 dihydrochloride) 是一种选择性，口服可生物利用且具有 ATP 竞争性的 ALK 酪氨酸激酶抑制剂，IC₅₀ 为 200 pM。Ceritinib dihydrochloride (LDK378 dihydrochloride) 还抑制 IGF-1R，InsR 和 STK22D，IC₅₀ 值分别为 8、7 和 23 nM。Ceritinib dihydrochloride (LDK378 dihydrochloride) 显示出良好的抗肿瘤效力。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：ALK  |  Insulin Receptor  |  IGF-1R

In Vitro: Ceritinib (LDK378) shows great anti-proliferative activity in Ba/F3-NPM-ALK and Karpas290 cells with IC₅₀ of 26.0 nM and 22.8 nM, compared with IC₅₀ of 319.5 nM and 2477 nM in Ba/F3-Tel-InsR and Ba/F3-WT cells.

In Vivo: Ceritinib (LDK378) is designed to reduce the possibility of forming reactive metabolites and shows undetectable levels of glutathione (GSH) adducts (<1%) in liver microsomes. Ceritinib (LDK378) has relatively good metabolic stability, with moderate CYP3A4 (Midazolam substrate) inhibition and hERG inhibition. Ceritinib (LDK378) exhibits low plasma clearance in animals (mouse, rat, dog and monkey) compared to liver blood flow, with the oral bioavailability of above 55% in mouse, rat, dog and monkey. Ceritinib (LDK378) induces a dose-dependent growth inhibition and tumor regression in the Karpas299 and H2228 rat xenograft models, with no body-weight loss. Ceritinib (LDK378) shows no impact on insulin levels or plasma glucose utilization in the mouse upon chronic dosing up to 100 mg/kg.

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