Inecalcitol TX 522|cas:163217-09-2|西域试剂

Inecalcitol TX 522,98.11%

产品编号：Bellancom-32344| CAS NO：163217-09-2| 分子式：C₂₆H₄₀O₃| 分子量：400.59

伊奈钙化醇（TX 522）是一种独特的维生素D3类似物，是一种口服活性维生素D受体（VDR）激动剂，Kd为0.53 nM。降钙醇可诱导细胞凋亡，具有较强的抗癌活性。

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货号	价格	库存与货期
Bellancom-32344	￥6500.00	杭州北京（现货）
Bellancom-32344	￥18000.00	杭州北京（现货）
Bellancom-32344	￥30000.00	杭州北京（现货）

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Inecalcitol TX 522

产品介绍

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， K_d为 0.53 nM。Inecalcitol 可诱导细胞凋亡 (apoptosis)，并具有有效的抗癌活性。

生物活性

Inecalcitol (TX 522), a unique vitamin D3 analog, is an orally active vitamin D receptor (VDR) agonist with a K_d of 0.53 nM. Inecalcitol can induce cell apoptosis and has potent anticancer activities^[4].

体外研究

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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

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.
Pharmacokinetic studies show that plasma half-life of Inecalcitol (C57Bl/6J mice; 1.3 mg/kg; i.p.) is 18.3 minutes in mice.

西域 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
Dosage:	1.3 mg/kg
Administration:	i.p.; 3 times per week; for 42 days
Result:	Inhibited androgen-responsive prostate cancer growth in vivo.

体内研究

西域 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
Dosage:	1.3 mg/kg
Administration:	i.p.; 3 times per week; for 42 days
Result:	Inhibited androgen-responsive prostate cancer growth in vivo.

体内研究

西域 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
Dosage:	1.3 mg/kg
Administration:	i.p.; 3 times per week; for 42 days
Result:	Inhibited androgen-responsive prostate cancer growth in vivo.

性状

Solid

溶解性数据

In Vitro:

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

配制储备液

浓度溶剂体积质量	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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

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

. 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. [Content Brief]

. 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. [Content Brief]

. 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. [Content Brief]

[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. [Content Brief]

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产品编号(Item Number)

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Inecalcitol TX 522,98.11%

Inecalcitol TX 522

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