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Alectinib

CAS No. : 1256580-46-7

MCE 国际站：Alectinib

产品活性：Alectinib (CH5424802) 是一种有效、选择性、具有口服活性的 ALK 抑制剂，其 IC₅₀ 为 1.9 nM，K_d 值为 2.4 nM (以 ATP 竞争方式)，并且还抑制 ALK F1174L 和 ALK R1275Q，其 IC₅₀ 分别为 1 nM 和 3.5 nM。Alectinib 还具有有效的中枢神经系统 (CNS) 渗透能力。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Anaplastic lymphoma kinase (ALK)

In Vitro: Alectinib (0-1000 nM; 2 hours; NCI-H2228 cells) treatment could prevent autophosphorylation of ALK in NCI-H2228 cells expressing EML4-ALK, and it also resulted in substantial suppression of phosphorylation of STAT3 and AKT.
?Alectinib (0-1000 nM; 5 days; HCC827, A549, or NCIH522 cells) treatment reduces cell activity in a dose-dependent manner.

In Vivo: Alectinib (0.2-20 mg/kg; oral administration; once daily; for 11 days; SCID or nude mice bearing NCI-H2228 cells) treatment can result in dose-dependent tumor growth inhibition (EC₅₀ of 0.46 mg/kg) and tumor regression. At any dose level, no differences in body weight or gross signs of toxicity are observed.

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