Inecalcitol  (Synonyms: TX 522)

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].

Kd: 0.53 nM (vitamin D receptor (VDR))^[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

400.59

Solid

C₂₆H₄₀O₃

163217-09-2

O[[email protected]]1C[[email protected]](O)C/C(C1)=C/C=C2[[email protected]@]3([H])CC[[email protected]]([[email protected]](C)CC#CC(C)(O)C)[[email protected]@]3(C)CCC/2

Room temperature in continental US; may vary elsewhere.

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

• [1]. Ryoko Okamoto, et al. Inecalcitol, an analog of 1α,25(OH)(2) D(3) , induces growth arrest of androgen-dependent prostate cancer cells. Int J Cancer. 2012 May 15;130(10):2464-73.  [Content Brief]

  [2]. L Verlinden, et al. Interaction of two novel 14-epivitamin D3 analogs with vitamin D3 receptor-retinoid X receptor heterodimers on vitamin D3 responsive elements. J Bone Miner Res. 2001 Apr;16(4):625-38.  [Content Brief]

  [3]. Jacques Medioni, et al. Phase I safety and pharmacodynamic of inecalcitol, a novel VDR agonist with docetaxel in metastatic castration-resistant prostate cancer patients. Clin Cancer Res. 2014 Sep 1;20(17):4471-7.  [Content Brief]

  [4]. Yingyu Ma, et al. Inecalcitol, an analog of 1,25D3, displays enhanced antitumor activity through the induction of apoptosis in a squamous cell carcinoma model system. Cell Cycle. 2013 Mar 1;12(5):743-52.  [Content Brief]