2. Cell Cycle/DNA Damage Cytoskeleton
  3. Microtubule/Tubulin
  4. Amphethinile

Amphethinile  (Synonyms: Amphetinile; CRC 82-07)

目录号: HY-100190
产品使用指南

摩尔计算器

Amphethinile是一种抗微管蛋白 (anti-tubulin) 剂。 Amphethinile与微管蛋白结合的Ka 值为1.3 μM。

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Amphethinile Chemical Structure

Amphethinile Chemical Structure

CAS No. : 91531-98-5

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Amphethinile 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Amphethinile is an anti-tubulin agent. The affinity constant for the association (Ka) of Amphethinile with tubulin is 1.3 μM.

IC50 & Target

Ka: 1.3 μM (Tubulin)[1]
体外研究
(In Vitro)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Amphethinile 相关抗体:
体内研究
(In Vivo)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

265.33

Formula

C15H11N3S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献
Cell Assay

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 (1O μM, 2h, 37°C) are performed in RPMI medium in the presence or absence of horse serum (10%). Cell suspensions (100 mL) are centrifuged (800 g, 10 min, 4°C), washed in PBS, lysed in distilled water by sonication, and the drug extracted into CHC13. The amphethinile concentration is determined spectrophotometrically (λ=304 nm) relative to a standard curve[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration

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 10 g amphethinile and 100 g Solutol HS15 diluted to 200 mL with 70% ethanolic citrate buffer at pH 6.0. The resulting drug concentration is 50mg mL [2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

Amphethinile 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Amphethinile91531-98-5Amphetinile CRC 82-07Microtubule/TubulinInhibitorinhibitorinhibit

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