Epothilone D
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:MCF-7细胞系为2.9 nM;KB-31细胞系为2.7 nM;CCRF-CEM细胞系为9.5 nM。
靶向微管的药物在人类恶性疾病中是有活性的,是药物治疗这些疾病的主要组分。因此,对于干扰微管功能的药物研究集中于可能增强药效或降低毒性的药剂。Epothilone D是一种更有效的微管稳定剂。
体外实验:Epothilone D比Epothilone A或B在稳定微管方面更有效。与紫杉醇功效类似,在一系列人肿瘤细胞系中,Epothilone D表现出较强的细胞毒性。在耐药细胞系中,Epothilone D也比紫杉醇更有优势,在过表达P-糖蛋白的多药耐药细胞系中能够保持其细胞毒性[1]。
体内试验:在紫杉醇敏感和耐药异种移植物以及包括耐多柔比星CCRF-CEM白血病细胞异种移植物在内的某些多药耐药移植物中,Epothilone D都表现出了抗肿瘤活性[1]。
临床试验:Epothilone D耐受性良好、毒性可控,较好的PK图谱以及临床活性。最大耐受剂量为100 mg/m2,给药3周停药1周。给予Epothilone D的病人外周血单核细胞中能观察到MTBF。
参考文献:
[1] Konner J, Grisham RN, Park J, O'Connor OA, Cropp G, Johnson R, Hannah AL, Hensley ML, Sabbatini P, Mironov S, Danishefsky S, Hyman D, Spriggs DR, Dupont J, Aghajanian C. Phase I clinical, pharmacokinetic, and pharmacodynamic study of KOS-862 (Epothilone D) in patients with advanced solid tumors and lymphoma. Invest New Drugs. 2012 Dec;30(6):2294-302. doi: 10.1007/s10637-011-9765-7.
Physical Appearance | A white to off-white solid |
Storage | Store at -20°C |
M.Wt | 491.68 |
Cas No. | 189453-10-9 |
Formula | C27H41NO5S |
Synonyms | 12,13-Desoxyepothilone B; Desoxyepothilone B; KOS 862 |
Solubility | Soluble in DMSO |
Chemical Name | (4S,7R,8S,9S,13Z,16S)-4,8-dihydroxy-5,5,7,9,13-pentamethyl-16-[(E)-1-(2-methyl-1,3-thiazol-4-yl)prop-1-en-2-yl]-1-oxacyclohexadec-13-ene-2,6-dione |
SDF | Download SDF |
Canonical SMILES | CC1CCCC(=CCC(OC(=O)CC(C(C(=O)C(C1O)C)(C)C)O)C(=CC2=CSC(=N2)C)C)C |
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。 |
动物实验 [1]: | |
动物模型 |
PS19小鼠 |
剂量 |
1mg/kg或3mg/kg,腹腔注射,每周一次,持续3个月 |
应用 |
接受低剂量Epothilone D治疗3个月的PS19小鼠营养不良性轴突显着减少,用3 mg / kg浓度的 Epothilone D 处理PS19小鼠,轴突营养不良情况也显著减轻,可能是由于微管的过度稳定所致。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。 |
References: [1]. Brunden KR, Zhang B, Carroll J, Yao Y, Potuzak JS, Hogan AM, Iba M, James MJ, Xie SX, Ballatore C, Smith AB 3rd, Lee VM, Trojanowski JQ. Epothilone D improves microtubule density, axonal integrity, and cognition in a transgenic mouse model of tauopathy. J Neurosci. 2010 Oct 13;30(41):13861-6. doi:10.1523/JNEUROSCI.3059-10.2010. PubMed PMID: 20943926; PubMed Central PMCID: PMC2958430. |
Description | Epothilone B是一种紫杉醇样微管稳定剂,其EC0.01值为1.8 μM。 | |||||
靶点 | Tubulin | |||||
IC50 | 1.8 μM(EC0.01) |