Cevipabulin
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.
Cevipabulin(TTI-237)是一种新型的抗微管药[1][2][3][4].
微管是细胞骨架成分,参与各种重要的细胞功能,包括维持细胞结构\形成细胞骨架以及染色体分离.
Cevipabulin(TTI-237)是一种新型的抗微管药,具有抗肿瘤活性.在COLO205细胞中,TTI-237抑制细胞增殖,其IC50值为31 nM[1].在TTI-237与微管蛋白异二聚体的比率(约1:30)较低时,TTI-237响应于低温而促进解聚反应动力学,但在较高比率(约1:4)下,TTI-237稳定聚合物.在微管蛋白异二聚体的核苷酸交换位点上,TTI-237抑制[3H]GTP交换[2].Cevipabulin(TTI-237)促进微管蛋白聚合.Cevipabulin具有稳定性与水溶性,可以溶于盐水中进行静脉注射或口服给药[3].TTI-237抑制[3H]Vinblastine结合微管蛋白,但显著增加了浊度(非常类似于Docetaxel的作用).在HeLa细胞中,TTI-237(34 nmol/L)诱导多极纺锤体以及多核细胞.20 ~ 40 nmol/L TTI-237诱导细胞出现亚G1期细胞核,而> 50 nmol/L TTI-237导致G2-M期阻滞.
在人结肠腺癌LoVo细胞异种移植无胸腺小鼠中,TTI-237呈剂量依赖性地对抗肿瘤.在人胶质母细胞瘤U87-MG细胞异种移植小鼠中,静脉注射和口服给予TTI-237(25 mg/kg)具有相等的疗效.[4].
参考文献：
[1]. Zhang N, Ayral-Kaloustian S, Nguyen T, et al. 2-cyanoaminopyrimidines as a class of antitumor agents that promote tubulin polymerization. Bioorg Med Chem Lett, 2007, 17(11): 3003-3005.
[2]. Beyer CF, Zhang N, Hernandez R, et al. The microtubule-active antitumor compound TTI-237 has both paclitaxel-like and vincristine-like properties. Cancer Chemother Pharmacol, 2009, 64(4): 681-689.
[3]. Ayral-Kaloustian S, Zhang N, Beyer C. Cevipabulin (TTI-237): preclinical and clinical results for a novel antimicrotubule agent. Methods Find Exp Clin Pharmacol, 2009, 31(7): 443-447.
[4]. Beyer CF, Zhang N, Hernandez R, et al. TTI-237: a novel microtubule-active compound with in vivo antitumor activity. Cancer Res, 2008, 68(7): 2292-2300.
| Storage | Store at -20°C |
| M.Wt | 464.82 |
| Cas No. | 849550-05-6 |
| Formula | C18H18ClF5N6O |
| Solubility | Soluble in DMSO |
| Chemical Name | (S)-5-chloro-6-(2,6-difluoro-4-(3-(methylamino)propoxy)phenyl)-N-(1,1,1-trifluoropropan-2-yl)-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine |
| SDF | Download SDF |
| Canonical SMILES | C[C@@](NC1=C(C(Cl)=NC2=NC=NN12)C3=C(F)C=C(OCCCNC)C=C3F)([H])C(F)(F)F |
| 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。 |
化学结构
