Inecalcitol

Inecalcitol (TX 522), a unique vitamin D3 analog, is an orally active vitamin D receptor (VDR) agonist with a Kd of 0.53 nM. Inecalcitol can induce cell apoptosis and has potent anticancer activities[1][2][3][4]. Inecalcitol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Product Specifications

CAS Number

[163217-09-2]

Product Name Alternative

TX 522

UNSPSC

12352211

Target

Apoptosis; VD/VDR

Type

Reference compound

Related Pathways

Apoptosis; Vitamin D Related/Nuclear Receptor

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/inecalcitol.html

Purity

98.11

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C26H40O3

Molecular Weight

400.59

References & Citations

[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.|[2]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.|[3]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.|[4]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.