13585831301
021-59541103 021-60443211
3004967995
13585831301021-59541103 021-604432113004967995
在線訂購 免費訂購熱線：021-59541103 021-60443211
聯系人:高小姐
電話:021-59541103 021-60443211
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詳細地址：上海嘉定區嘉羅公路1661
化學性質：
| 規格 | 1mg 5mg 10mg |
| CAS | 91531-98-5 |
| 別名 | N/A |
| 化學名 | N/A |
| 分子式 | C15H11N3S |
| 分子量 | 265.33 |
| 溶解度 | Soluble in DMSO |
| 儲存條件 | 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 |
產品描述：
Amphethinile is an anti-tubulin agent. The affinity constant for the association (Ka) of Amphethinile with tubulin is 1.3 μM.
Amphethinile shows a remarkable similarity to colchicine in terms of its binding to tubulin and inhibition of microtubular assembly. Amphethinile binds strongly to microtubule protein (Ka=1.3 μM). This interaction has been shown to be capable of inhibiting tubulin assembly, but shows no rapid stimulation of disassembly when added to assembled tubulin. The concentration of amphethinile required to inhibit assembly by 50% (12 μM) is very similar to that for colchicine (11 μM). Amphethinile has been shown to be capable of competing for colchicine binding sites but not for those of the vinca alkaloids. Amphethinile can also be shown to stimulate the GTPase activity of tubulin in a manner similar to that observed for combretastatin A4 and 2-methoxy-5-(2',3',4'-trimethoxyphenyl) tropolone (MTPT)[1]. Amphethinile has been shown to cause a G2/M phase block in the cell cycle. In addition, this agent has been shown to be equally toxic toward parental and daunorubicin-resistant P388 cells. Whereas resistance in this cell line is associated with decreased drug accumulation in the case of daunorubicin, vincristine and vinblastine, this effect is much less pronounced for amphethinile[2].
Pharmacokinetic studies in male mice are undertaken. Area under the curve values (AUC), show that levels of 313 μg/L per hour are attained at doses equivalent to the LD10. The alpha half life is 8 min after a bolus intravenous injection. The beta half life is 100 min and relatively independent of dose level[2].
[1]. McGown AT, et al. Interaction of the novel agent amphethinile with tubulin. Br J Cancer. 1989 Jun;59(6):865-8. [2]. McGown AT, et al. Pre-clinical studies of a novel anti-mitotic agent, amphethinile. Br J Cancer. 1988 Feb;57(2):157-9.
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原創作者：上海莼試生物技術有限公司
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賬 戶 名：上海生物
開 戶 行：中國銀行山東省分行營業部
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