生物活性

Paclitaxel is a novel antineoplastic agent, which was discovered in a screen of extracts of thousands of plants and natural products for antineoplastic activity by a National Cancer Institute program. Alought it functions as a mitotic inhibitor like vinca alkaloids, paclitaxel promotes the polymerization of tubulin instead of inducing the disassembly of microtubules, which inhibits the microtubules disassembly and promotes the formation of excessively stable, dysfunctional microtubules. Paclitaxel has exhibited antitumor activity against a broad spectrum of human cancers, including ovarian, breast, head and neck, and lung cancer, in a large number of studies.

体外研究

体内研究

1% DMSO+30% polyethylene glycol+1% Tween 80

激酶实验

细胞实验

0.1 pM-100 pM

动物实验

20 mg/kg 静脉注射

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

参考文献

[1] Wang J, et al. Anticancer Drugs. 2003, 14(1), 13-19.
[2] McGuire et al (1989) Taxol: a unique antineoplastic agent with significant activity in advanced ovarian epithelial neoplasms. Ann.Intern.Med. 111 273.
[3] Rao et al (1999) Characterization of the taxol binding site on the microtubule. J.Biol.Chem. 274 37990.
[4] Park et al (2004) Taxol induces caspase-10-dependent apoptosis. J.Biol.Chem. 279 51057.
[5] Rowinsky et al (1990) Taxol: a novel investigational antimicrotubule agent. J.Natl.Cancer Inst. 82 1247.

体内溶解度

Clinical Trial Information ( data from http://clinicaltrials.gov )

注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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