1. Vitamin D Related/Nuclear Receptor Apoptosis
  2. VD/VDR Apoptosis
  3. Inecalcitol

Inecalcitol  (Synonyms: TX 522)

Cat. No.: HY-32344
Handling Instructions

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. 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.

For research use only. We do not sell to patients.

Inecalcitol Chemical Structure

Inecalcitol Chemical Structure

CAS No. : 163217-09-2

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Description

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.

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].

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

Western Blot Analysis[1]

Cell Line: LNCaP cells
Concentration: 0.1 nM, 1 nM, 10 nM
Incubation Time: 48 hours
Result: Resulted in decreased expression of both protein and mRNA of Pim-1 in a dose-dependent manner.
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].

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

Animal Model: Male BNX nu/nu mice (8 weeks of age) injected with LNCaP cells[1]
Dosage: 1.3 mg/kg
Administration: i.p.; 3 times per week; for 42 days
Result: Inhibited androgen-responsive prostate cancer growth in vivo.
Clinical Trial
Molecular Weight

400.59

Formula

C26H40O3

CAS No.
Appearance

Solid

Color

Off-white to light yellow

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (249.63 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4963 mL 12.4816 mL 24.9632 mL
5 mM 0.4993 mL 2.4963 mL 4.9926 mL
10 mM 0.2496 mL 1.2482 mL 2.4963 mL
*Please refer to the solubility information to select the appropriate solvent.
Purity & Documentation
References
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Inecalcitol Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Inecalcitol
Cat. No.:
HY-32344
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