Inecalcitol

Inecalcitol (TX 522), a unique vitamin D3 analog, is an orally active vitamin D receptor (VDR) agonist with a K_d of 0.53 nM. Inecalcitol can induce cell apoptosis and has potent anticancer activities^[1][2][3][4]. Inecalcitol is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. IC50 & Target: Kd: 0.53 nM (vitamin D receptor (VDR))^[2] 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^[1].
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^[1]. In Vivo: Inecalcitol (1.3 mg/kg; i.p.; 3 times per week; for 42 days) inhibits androgen-responsive prostate cancer growth in vivo^[1].
Pharmacokinetic studies show that plasma half-life of Inecalcitol (C57Bl/6J mice; 1.3 mg/kg; i.p.) is 18.3 minutes in mice^[1].