產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 5mg 10mg 50mg 100mg
CAS	849550-05-6
別名	N/A
化學(xué)名	(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
分子式	C18H18ClF5N6O
分子量	464.82
溶解度	Soluble in DMSO
儲(chǔ)存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

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].

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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