| 中文名称: | Amphethinile | ||||
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| 英文名称: | Amphethinile | ||||
| 别名: | Amphetinile; CRC 82-07 | ||||
| CAS No: | 91531-98-5 | 分子式: | C15H11N3S | 分子量: | 265.33 |
| CAS No: | 91531-98-5 | ||||
| 分子式: | C15H11N3S | ||||
| 分子量: | 265.33 | ||||
基本信息
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产品编号：A11392 |
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产品名称：Amphethinile |
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CAS: |
91531-98-5 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
265.33 |
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化学名： |
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Solubility (25°C) |
体外 |
DMSO |
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Ethanol |
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Water |
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体内（现配现用） |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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生物活性
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产品描述 |
一种抗微管蛋白 (anti-tubulin) 剂。 Amphethinile与微管蛋白结合的Ka 值为1.3μM。 |
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靶点/IC50 |
Ka: 1.3μM (Tubulin) |
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体外研究 |
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=1.3μM). 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% (12μM) is very similar to that for colchicine (11μM).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). 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. |
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体内研究 |
Pharmacokinetic studies in male mice are undertaken. Area under the curve values (AUC), show that levels of 313μg/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. |
推荐实验方法(仅供参考)
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细胞实验: |
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The volume of methanol in the final incubation mixture is <1%, which does not modify the uptake of any of the drugs used in either drug sensitive or resistant lines. In addition, the same level of methanol is used in the control cultures. Drug incubations (1OμM, 2h, 37℃) are performed in RPMI medium in the presence or absence of horse serum (10%). Cell suspensions (100mL) are centrifuged (800g,10 min,4℃), washed in PBS, lysed in distilled water by sonication,and the drug extracted into CHC13. The amphethinile concentration is determined spectrophotometrically (λ=304nm) relative to a standard curve. |
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动物实验: |
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Mouse: Initial toxicity studies on this agent are performed under contract in MFI-strain male mice following an acute i.v. and i.p.administration as well as a 4-weekly 5 day sub acute study.Preclinical toxicology is undertaken using the clinically formulated drug. The formulation consisted of 10g amphethinile and 100g Solutol HS15 diluted to 200mL with70% ethanolic citrate buffer at pH 6.0. The resulting drug concentration is 50mg mL. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
