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Inecalcitol
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Inecalcitol图片
CAS NO:163217-09-2
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品名称
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，Kd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 activevitamin D receptor (VDR)agonist with aKdof 0.53 nM. Inecalcitol can induce cellapoptosisand 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 ED50values of 4.0 nM and 0.28 nM, respectively[1].

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].

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

性状

Solid

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)

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 mg5 mg10 mg
1 mM2.4963 mL12.4816 mL24.9632 mL
5 mM0.4993 mL2.4963 mL4.9926 mL
10 mM0.2496 mL1.2482 mL2.4963 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℃, 6 months; -20℃, 1 month (protect from light, stored under nitrogen)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。