Inecalcitol(Synonyms: TX 522)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Inecalcitol (Synonyms: TX 522) 纯度: 98.11%

Inecalcitol (TX 522)，一种独特的维生素 D3 类似物，是一种具有口服活性维生素 D 受体 (VDR) 激动剂， Kd 为 0.53 nM。Inecalcitol 可诱导细胞凋亡 (apoptosis)，并具有有效的抗癌活性。

Inecalcitol(Synonyms: TX 522)

Inecalcitol Chemical Structure

CAS No. : 163217-09-2

规格 价格 是否有货 数量
1 mg ￥6500 In-stock
5 mg ￥18000 In-stock
10 mg ￥30000 In-stock
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Inecalcitol 相关产品

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生物活性

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].

IC50 & Target

Kd: 0.53 nM (vitamin D receptor (VDR))[2]
体外研究
(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].

上海金畔生物科技有限公司 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.

体内研究
(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].

上海金畔生物科技有限公司 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

分子量

400.59

Formula

C26H40O3
CAS 号

163217-09-2
中文名称

伊奈骨化醇；依奈骨化醇
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light, stored under nitrogen

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

  • [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]. 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.

    [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.

    [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.

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