2. Vitamin D Related/Nuclear Receptor Apoptosis
  3. VD/VDR Apoptosis
  4. 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. 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.

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Inecalcitol Chemical Structure

Inecalcitol Chemical Structure

CAS No. : 163217-09-2

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Based on 1 publication(s) in Google Scholar

Inecalcitol Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Inecalcitol

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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.

Inecalcitol Related Antibodies

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

-20°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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4963 mL 12.4816 mL 24.9632 mL 62.4079 mL
5 mM 0.4993 mL 2.4963 mL 4.9926 mL 12.4816 mL
10 mM 0.2496 mL 1.2482 mL 2.4963 mL 6.2408 mL
15 mM 0.1664 mL 0.8321 mL 1.6642 mL 4.1605 mL
20 mM 0.1248 mL 0.6241 mL 1.2482 mL 3.1204 mL
25 mM 0.0999 mL 0.4993 mL 0.9985 mL 2.4963 mL
30 mM 0.0832 mL 0.4161 mL 0.8321 mL 2.0803 mL
40 mM 0.0624 mL 0.3120 mL 0.6241 mL 1.5602 mL
50 mM 0.0499 mL 0.2496 mL 0.4993 mL 1.2482 mL
60 mM 0.0416 mL 0.2080 mL 0.4161 mL 1.0401 mL
80 mM 0.0312 mL 0.1560 mL 0.3120 mL 0.7801 mL
100 mM 0.0250 mL 0.1248 mL 0.2496 mL 0.6241 mL
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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.

Keywords:

Inecalcitol163217-09-2TX 522TX522TX-522VD/VDRApoptosisVitamin DVitamin D receptorantiproliferativeETV1anticancerPim-1VDR,Inhibitorinhibitorinhibit

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