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| Cas No.: | 163217-09-2 |
| Chemical Name: | Inecalcitol |
| SMILES: | O[C@H]1C[C@H](O)C/C(C1)=C\C=C2[C@@H](CC[C@@H]3[C@H](C)CC#CC(C)(O)C)[C@]3(C)CCC\2 |
| Formula: | C26H40O3 |
| M.Wt: | 400.59 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | 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]. |
| Target: | Kd: 0.53 nM (vitamin D receptor (VDR))[2] |
| In Vivo: | 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]. 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. |
| 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]. 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. |
| References: | [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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COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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