Inecalcitol 是一种独特的维生素 D3 类似物，可诱导细胞凋亡，有抗癌活性。它是一种具有口服活性维生素 D 受体激动剂，Kd为 0.53 nM。

Inecalcitol is the growth inhibitor of human breast cancer cells. Inecalcitol is a unique vitamin D3 analog with Kd of 0.53 nM.

A xenograft model of LNCaP cells was developed in immunodeficient mice treated with inecalcitol. The tumors of the diluent-treated control mice increased in size but those in the inecalcitol treatment group did not grow[1].

Inecalcitol maximal tolerated dose (MTD) by intraperitoneal (i.p.) administration was 30 μg/mouse (1,300 μg/kg) three times per week, while we previously found that the MTD of 1,25(OH)(2) D(3) is 0.0625 μg/mouse; therefore, inecalcitol is 480 times less hypercalcemic than 1,25OH2 D3[1]. Inecalcitol inhibits androgen-responsive prostate cancer growth in vivo.

163217-09-2

C26H40O3

400.59

TX-522;伊奈骨化醇;TX 522;TX522;Inecalcitol

DMSO:55 mg/ml (137.3 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years