Inecalcitol伊奈骨化醇,163217-09-2

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Inecalcitol

CAS No. : 163217-09-2

MCE 国际站：Inecalcitol

产品活性：Inecalcitol (TX 522)，一种独特的维生素 D3 类似物，是一种具有口服活性维生素 D 受体 (VDR) 激动剂， K_d 为 0.53 nM。Inecalcitol 可诱导细胞凋亡 (apoptosis)，并具有有效的抗癌活性。

研究领域：Vitamin D Related/Nuclear Receptor  |  Apoptosis

作用靶点：VD/VDR  |  Apoptosis

In Vitro: Inecalcitol (0.1-10 nM; 48 hours) treatment of LNCaP cells results in decreased expression of both protein and mRNA of Pim-1 in a dose-dependent manner. Inecalcitol (0.1-10 nM; 48 hours) also decreases ETV1 expression levels in a dose-dependent manner.
Inecalcitol (10-14 days) inhibits the growth of LNCaP and HL-60 cells with ED₅₀ values of 4.0 nM and 0.28 nM, respectively.

In Vivo: Inecalcitol (1.3 mg/kg; i.p.; 3 times per week; for 42 days) inhibits androgen-responsive prostate cancer growth in vivo.
Pharmacokinetic studies show that plasma half-life of Inecalcitol (C57Bl/6J mice; 1.3 mg/kg; i.p.) is 18.3 minutes in mice.

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