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Amphethinile

Catalog No. T10309 CAS 91531-98-5

Synonyms: Amphetinile, CRC 82-07

Amphethinile is an anti-tubulin agent. The Ka of Amphethinile with tubulin is 1.3 μM.

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Amphethinile, CAS 91531-98-5

Pack Size	Availability	Price/USD
25 mg	6-8 weeks	$ 1,520.00
50 mg	6-8 weeks	$ 1,980.00
100 mg	6-8 weeks	$ 2,500.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Amphethinile is an anti-tubulin agent. The Ka of Amphethinile with tubulin is 1.3 μM.
Targets&IC50	Tubulin: 1.3 μM (Ka)
In vitro	Amphethinile exhibits strong binding affinity to microtubule proteins (Ka=1.3 µM) and effectively inhibits the assembly of tubulin without promoting its rapid disassembly. Its inhibitory concentration for assembly (12 μM) closely matches that of colchicine (11 μM), and it competes for the same binding sites as colchicine, though not for those targeted by vinca alkaloids. Furthermore, amphethinile enhances the GTPase activity of tubulin, akin to the effects observed with combretastatin A4 and 2-methoxy-5-(2',3',4'-trimethoxyphenyl) tropolone (MTPT). It causes a G2/M phase block in the cell cycle and demonstrates equal toxicity towards both parental and daunorubicin-resistant P388 cells. Unlike daunorubicin, vincristine, and vinblastine, where resistance in P388 cells is linked to reduced drug accumulation, amphethinile's effectiveness is less affected by such resistance mechanisms.
In vivo	Pharmacokinetic studies in male mice are undertaken. The AUC shows 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 the dose level [2].

Synonyms	Amphetinile, CRC 82-07
Molecular Weight	265.33
Formula	C15H11N3S
CAS No.	91531-98-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Amphethinile 91531-98-5 Others Amphetinile CRC 82-07 inhibitor inhibit

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