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Inecalcitol

SKU: orb1305513

Description

Inecalcitol is a potent, orally active vitamin D receptor agonist (Kd = 0.53 nM). This unique vitamin D3 analog exhibits anticancer properties by inducing apoptosis, making it a valuable tool for research in oncology, both in vitro and in vivo.

Research Area

Cell Biology, Metabolism Research

Images & Validation

Key Properties

CAS Number163217-09-2
MW400.59
Purity99.96%
FormulaC26H40O3
SMILES[H][C@]12CC[C@H]([C@H](C)CC#CC(C)(C)O)[C@@]1(C)CCC\C2=C/C=C1C[C@@H](O)C[C@H](O)C1
TargetApoptosis,Vitamin
SolubilityDMSO:55 mg/mL (137.3 mM)

Bioactivity

Target IC50
Vitamin D3:0.53 nM(Kd)
In Vivo
METHODS: Inecalcitol (TX 522) (1.3 mg/kg, intraperitoneal injection, 3 times a week) was used to treat mice bearing LNCaP cell tumor xenografts. Tumor size was measured and calculated, and blood was collected to measure serum calcium levels. RESULTS Inecalcitol-treated mice bearing tumor xenografts had a significant reduction in tumor size. The half-life of plasma Inecalcitol was 18.3 minutes.
In Vitro
METHODS: SCC cells were treated with Inecalcitol (TX 522) (0.0008, 0.003, 0.012, 0.05, 0.2, 0.8, 3.2, 12.5 nM, 48 hours) and cell viability was measured by MTT assay. RESULTS Inecalcitol inhibited the growth of SCC cells in a dose-dependent manner with an IC50 of 0.38 nM. METHODS: SCC cells were treated with Inecalcitol (TX 522) (1,10 nM), and Western Blot analysis was used to investigate the mechanism of inecalcitol-induced apoptosis. RESULTS Inecalcitol-treated SCC cells resulted in increased activity of caspase 8, 10, and 3, indicating that inecalcitol promotes apoptosis by activating the extrinsic pathway mediated by caspase 8/10 and caspase 3.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Apoptosis, antiproliferative, anticancer, ETV1, Inhibitor, Inecalcitol, inhibit, Pim-1, TX 522, TX522, TX-522, VDR, VD/VDR, Vitamin D, Vitamin D receptor
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Key Properties

No computed properties available.

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Inecalcitol (orb1305513)

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Step 1: Enter information below

(Recommended: An additional animal making an allowance for loss during the experiment)

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% DMSO +
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% Tween 80 +
%

Available Sizes

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1 mg
¥ 1,170.00
5 mg
¥ 2,080.00
1 ml x 10 mM (in DMSO)
¥ 2,210.00
10 mg
¥ 2,990.00
25 mg
¥ 6,240.00