Inecalcitol
Based on 1 publication(s) in Google Scholar
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. Inecalcitol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- 純度: 98.44%
- CAS 番号: 163217-09-2
- 分子式: C26H40O3
- 分子量:400.59
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保管条件:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Inecalcitol
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生物活性
Kd: 0.53 nM (vitamin D receptor (VDR))[2]
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LNCaP cells
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Concentration:0.1 nM, 1 nM, 10 nM
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Incubation Time:48 hours
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Result:Resulted in decreased expression of both protein and mRNA of Pim-1 in a dose-dependent manner.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male BNX nu/nu mice (8 weeks of age) injected with LNCaP cells[1]
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Dosage:1.3 mg/kg
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Administration:i.p.; 3 times per week; for 42 days
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Result:Inhibited androgen-responsive prostate cancer growth in vivo.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 163217-09-2
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性状 Solid
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分子量 400.59
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分子式 C26H40O3
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Color Off-white to light yellow
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SMILES
O[C@H]1C[C@H](O)C/C(C1)=C/C=C2[C@@]3([H])CC[C@H]([C@H](C)CC#CC(C)(O)C)[C@@]3(C)CCC/2
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別名
TX 522
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Publications (1)
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Journal Impact Factor
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Most Recent
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Virol Sin
Antiviral activity of vitamin D derivatives against severe fever with thrombocytopenia syndrome virus in vitro and in vivo. [Abstract]2024 Aug 19:S1995-820X(24)00134-2. PMID: 39168248
溶剤 & 溶解度
DMSO : 100 mg/mL (249.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[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. [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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4963 mL | 12.4816 mL | 24.9632 mL | 62.4079 mL |
| 5 mM | 0.4993 mL | 2.4963 mL | 4.9926 mL | 12.4816 mL | |
| 10 mM | 0.2496 mL | 1.2482 mL | 2.4963 mL | 6.2408 mL | |
| 15 mM | 0.1664 mL | 0.8321 mL | 1.6642 mL | 4.1605 mL | |
| 20 mM | 0.1248 mL | 0.6241 mL | 1.2482 mL | 3.1204 mL | |
| 25 mM | 0.0999 mL | 0.4993 mL | 0.9985 mL | 2.4963 mL | |
| 30 mM | 0.0832 mL | 0.4161 mL | 0.8321 mL | 2.0803 mL | |
| 40 mM | 0.0624 mL | 0.3120 mL | 0.6241 mL | 1.5602 mL | |
| 50 mM | 0.0499 mL | 0.2496 mL | 0.4993 mL | 1.2482 mL | |
| 60 mM | 0.0416 mL | 0.2080 mL | 0.4161 mL | 1.0401 mL | |
| 80 mM | 0.0312 mL | 0.1560 mL | 0.3120 mL | 0.7801 mL | |
| 100 mM | 0.0250 mL | 0.1248 mL | 0.2496 mL | 0.6241 mL |
Inecalcitol 関連分類
HY-32344 関連分類
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