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Ceritinib

CAS No. : 1032900-25-6

MCE 站：Ceritinib

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

研究领域：Protein Tyrosine Kinase/RTK

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

In Vitro: Ceritinib (LDK378) also inhibits RET (IC₅₀=400 nM), FGFR3 (IC₅₀=430 nM), LCK (IC₅₀=560 nM), JAK2 (IC₅₀=610 nM), Aurora (IC₅₀=660 nM), LYN (₅₀=840 nM), EGFR (IC₅₀=900 nM), and FGFR4 (IC₅₀=950 nM). Ceritinib (LDK378) retains high potency against the ALK enzymatic activity with an IC₅₀ value of 200 pM and shows only strong inhibition against IGF-1R, InsR, and STK22D out of a panel of 46 kinases with a minimum selectivity of 70-fold. In Ba/F3 cells transfected with various kinases, Ceritinib inhibits ALK activity with an IC₅₀ value of 40.7 nM and had IC₅₀ values of >100 nM against all other kinases tested. Ceritinib (LDK378) shows potent antiproliferative activity with an IC₅₀ value of 22.8 nM in Karpas 299 human non-Hodgkin’s K_i-positive large cell lymphoma carrying the NPM-ALK fusion gene and 26 nM in Ba/F3 cells transfected with the NPM-ALK fusion gene. Ceritinib also shows good selectivity over wild-type Ba/F3 cells (IC₅₀>2 μM) and Ba/F3 cells transfected with Tel-InsR gene (IC₅₀=320 nM).

In Vivo: Ceritinib (LDK378) has an excellent pharmacokinetics profile in rodents and non-rodents with an oral bioavailability of >50%. Ceritinib demonstrates dose-dependent tumor growth inhibition and achieved partial tumor regression in the Karpas 299 rat xenograft model with daily administration but is capable of achieving complete tumor regression in the H2228 NSCLC rat xenograft model, which carries the EML4-ALK fusion gene. In both models, Ceritinib (LDK378) is well tolerated in animals. Ceritinib (LDK378) is further assessed for its ADME profile and is found to have a relatively good metabolic stability in liver microsomes, modest CYP3A4 inhibition, some hERG inhibition with an IC₅₀ value of 46 μM in hERG patch clamp experiments, but no evidence of QTc prolongation in both dog and monkey telemetry studies.

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