| CevipabulinAnti-microtubule agent |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 98.00%
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| Cas No. | 849550-05-6 | SDF | Download SDF |
| 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 | ||
| Canonical SMILES | C[C@@](NC1=C(C(Cl)=NC2=NC=NN12)C3=C(F)C=C(OCCCNC)C=C3F)([H])C(F)(F)F | ||
| Formula | C18H18ClF5N6O | M.Wt | 464.82 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Cevipabulin (TTI-237) is a new anti-microtubule agent [1][2][3][4].
Microtubules are a component of the cytoskeleton that participate in many crucial cellular functions, include maintaining the structure of the cell, forming the cytoskeleton and chromosome separation.
Cevipabulin (TTI-237) is a new anti-microtubule agent with antitumor activity. In COLO 205 cells, TTI-237 inhibited cell proliferation with IC50 value of 31 nM [1]. At low ratios of TTI-237: tubulin heterodimer (about 1:30), TTI-237 increased depolymerization kinetics in response to low temperature, but stabilized the aggregates at high ratios (about 1:4). TTI-237 inhibited the exchange of [3H]GTP at the exchangeable nucleotide site of the tubulin heterodimer [2]. Cevipabulin (TTI-237) increased tubulin polymerization. Cevipabulin was stable and water-soluble, and could be administered i.v. or p.o. in saline [3]. TTI-237 inhibited the binding of [3H]vinblastine to tubulin, but significantly increased turbidity development that more closely resembled the effect of docetaxel. In Hela cells, TTI-237 (34 nmol/L) induced multiple spindle poles and multi-nuclear cells. At 20-40 nmol/L, TTI-237 produced sub-G1 nuclei, while at > 50 nmol/L, TTI-237 induced G2-M block.
In athymic mice bearing LoVo human colon adenocarcinoma, TTI-237 exhibited good antitumor activity in a dose-dependent way. In mice bearing U87-MG human glioblastoma, TTI-237 (25 mg/kg) given both i.v. and p.o. were equally effective [4].
References:[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.
