Inecalcitol|163217-09-2|(TX 522)-陌孚医药/Medlife

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Inecalcitol (Synonyms: TX 522)

目录号: PL12558 纯度: ≥98%

CAS No. :163217-09-2

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中文名称	Inecalcitol
中文别名	依奈骨化醇;伊奈骨化醇;乳化剂E1302.E1306
英文名称	Inecalcitol
英文别名	Inecalcitol;(7E)-19-Nor-9,10-seco-14b-cholesta-5,7-dien-23-yne-1a,3b,25-triol;(1R,3R)-5-[(2E)-2-[(1R,3aR,7aR)-1-[(2R)-6-hydroxy-6-methylhept-4-yn-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]cyclohexane-1,3-diol;Ridinilazole;1,3-Cyclohexanediol,5-[(2E)-2-[(1R,3aR,7aR)-octahydro-1-[(1R)-5-hydroxy-1,5-diMethyl-3-hexyn-1-yl]-7a-Methyl-4H-inden-4-ylidene]ethylidene]-,(1R,3R)-;217I092;(1R,3R)-5-[(2E)-2-[(1R,3As,7aR)-1-[(2R)-6-hydroxy-6-methylhept-4-yn-2-yl]-7a-methyl-2,3,3a,5,6,7-hex
Cas No.	163217-09-2
分子式	C₂₆H₄₀O₃
分子量	400.59
包装储存	4°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

产品详情

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.

性状

Solid

IC50 & Target[1][2]

Kd: 0.53 nM (vitamin D receptor (VDR))

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

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

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)

ClinicalTrial

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.

溶解度数据	In Vitro: DMSO : 100 mg/mL (249.63 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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