Seocalcitol
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50值:在SKHEP-1细胞中,西奥骨化醇的IC50值为460.99 nM.
骨化三醇受体,也称维生素D受体(VDR),是转录因子核受体家族的成员.维生素D受体不仅调节转录反应,而且参与microRNA介导的转录后机制.西奥骨化醇(EB1089)是一种维生素D类似物,已受到广泛研究,且能显著地减少高血钙的影响.
体外实验:在之前的体外实验中发现,在所有检测过的西奥骨化醇浓度中,西奥骨化醇可显著抑制Hep 3B\PLC/PRF/5及SKHEP-1肝癌细胞(HCC)的细胞增殖,但HTC细胞仅对浓度为1,000 nM的EB1089有反应.然而,在所有检测过的浓度中,Novikoff细胞增殖不受该药物的影响[1].另一个体外细胞研究表明,EB1089显著抑制HEp-2细胞增殖,增加p57 mRNA和蛋白水平,这被siRNA-p57而非siRNA-con所阻断[2].
体内:西奥骨化醇有效抑制SKHEP-1肿瘤生长而不诱发高钙血症(p<0.05).这些结果表明,西奥骨化醇是一种有效的肝细胞癌肿瘤生长抑制剂[1].
临床实验:对患有不能手术切除的晚期肝细胞癌的56名患者进行长达一年的非受控口服西奥骨化醇研究.在具有可评价肿瘤反应的33名患者中,2名有完全反应(CR),12名病情稳定,19名疾病有所进展.治疗6至24个月后出现完全反应,该反应持续了29个月,至少36个月.西奥骨化醇耐受性良好,最常见的毒性是高钙血症及相关症状.大多数患者对西奥骨化醇的耐受剂量为每日10毫克.这些数据表明,特别在疾病早期,可以长期治疗的情况下,西奥骨化醇对治疗肝细胞癌有疗效.应在控制研究中确定具有或不具有肿瘤反应的存活率[3].
参考文献:
[1] Ghous Z, Akhter J, Pourgholami MH, Morris DL. Inhibition of hepatocellular cancer by EB1089: in vitro and in vive study. Anticancer Res. 2008;28(6A):3757-61.
[2] Lu L, Qiu J, Liu S, Luo W. Vitamin D3 analogue EB1089 inhibits the proliferation of human laryngeal squamous carcinoma cells via p57. Mol Cancer Ther. 2008;7(5):1268-74.
[3] Dalhoff K1 Dancey J, Astrup L, Skovsgaard T, Hamberg KJ, Lofts FJ, Rosmorduc O, Erlinger S, Bach Hansen J, Steward WP, Skov T, Burcharth F, Evans TR. A phase II study of the vitamin D analogue Seocalcitol in patients with inoperable hepatocellular carcinoma. Br J Cancer. 2003 21;89(2):252-7.
Physical Appearance | White lyophilised solid |
Storage | Store at -20°C |
M.Wt | 454.7 |
Cas No. | 134404-52-7 |
Formula | C30H46O3 |
Synonyms | EB 1089; EB-1089; EB1089 |
Solubility | Soluble in DMSO |
Chemical Name | (1R,3S,5E)-5-[(2Z)-2-[(1R,3aS,7aR)-1-[(2R,3E,5E)-7-ethyl-7-hydroxynona-3,5-dien-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol |
SDF | Download SDF |
Canonical SMILES | CCC(CC)(C=CC=CC(C)C1CCC2C1(CCCC2=CC=C3CC(CC(C3=C)O)O)C)O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Description | 作为骨化三醇的类似物,西奥骨化醇(seocalcitol)(EB 1089; EB-1089)是维生素D受体(VDR)的激动剂. | |||||
靶点 | VDR | |||||
IC50 |