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Tasidotin hydrochloride

产品编号 T16997 CAS 623174-20-9

别名: ILX651

Tasidotin hydrochloride is a peptide analog of the antimitotic depsipeptide dolastatin 15. Tasidotin hydrochloride is an inhibitor of microtubule assembly and microtubule dynamics.

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Tasidotin hydrochloride Chemical Structure

Tasidotin hydrochloride, CAS 623174-20-9

规格	价格/CNY		货期	数量
100 mg	待询		待询
500 mg	待询		待询

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Tasidotin hydrochloride is a peptide analog of the antimitotic depsipeptide dolastatin 15. Tasidotin hydrochloride is an inhibitor of microtubule assembly and microtubule dynamics.
体外活性	The greatest difference in sensitivity to Tasidotin is between the more sensitive MDA-MB-435 line and the less sensitive HS 578-T line of the remaining lines. The IC50 values in the two lines are 4 and 200 nM, respectively. The IC50 in Ewing's sarcoma, rhabdomyosarcoma, osteosarcoma, and synovial sarcoma lines ranges from 2 to 320 nM. Tasidotin induces a G2-M arrest that persists for 48 h after Tasidotin is washed from the cells in the SK-ES1 and RH30 cell lines. In vitro, more than half the cells are in the early or late phase of apoptosis 48 h after treatment with Tasidotin. Following treatment for 24 h with 160 nM Tasidotin, the RH30 line, and SK-ES1 line each shows an accumulation of cells in the G2-M phase. At hour 24, nearly all the RH30 cells are in the G2-M phase [1][2].
体内活性	Tasidotin (90 mg/kg/d, mice) treatment has a mean weight loss of <16% following each 5-day treatment of Tasidotin. In vivo, a significant increase in apoptotic nuclei is apparent in xenograft tumors harvested within 24 h after a 5-day course of Tasidotin. Mice treated with 100 mg/kg have a mean weight loss of >20% with no return to their baseline starting weight, and one mouse dies before the second treatment course [2].

别名	ILX651
分子量	643.3
分子式	C32H59ClN6O5
CAS No.	623174-20-9

存储

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

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参考文献

1. Bai R, et al. Intracellular activation and deactivation of Tasidotin, an analog of dolastatin 15: correlation with cytotoxicity. Mol Pharmacol. 2009 Jan;75(1):218-26. 2. Garg V, et al. Preclinical analysis of Tasidotin HCl in Ewing's sarcoma, rhabdomyosarcoma, synovial sarcoma, and osteosarcoma. Clin Cancer Res. 2007 Sep 15;13(18 Pt 1):5446-54.

剂量换算

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请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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