Paclitaxel 是一种从太平洋紫杉树皮中分离出来的环癸烷。 它以聚合形式稳定微管，导致细胞死亡。

Paclitaxel is a cyclodecane isolated from the bark of the Pacific yew tree. It stabilizes microtubules in their polymerized form leading to cell death.

Paclitaxel (0.1, 0.5, and 1 μM) dose-dependently reduces the proliferation and survival of CCRF-HSB-2 cells (IC50: 0.25 μM) [1]. Tested against a panel of cervical (HeLa), lung (A549), breast (MCF-7), colon (HT-29), ovarian (OVG-1), and pancreatic (PC-Sh) carcinomas, paclitaxel demonstrates IC50 values ranging from 2.5-7.5 nM [5]. Paclitaxel directly associates with the endoplasmic reticulum to stimulate the release of calcium into the cytosol, contributing to the induction of apoptosis [2].

In a SCID mouse xenograft model, low dose metronomic Paclitaxel treatment decreases lung dissemination of EGI-1 cells without significantly affecting their local tumor growth [3]. Paclitaxel (2 mg/kg per treatment, black circles) induces mechanical hypersensitivity in the glabrous skin of the hindpaw [4].

To determine which caspases are involved in apoptosis induced by taxol, caspase-3 inhibitor (DEVD-CHO), caspase-6 inhibitor (Z-VEID-FMK), caspase-8 inhibitor (Z-IETD-FMK or IETD-CHO), caspase-9 inhibitors (Z-LEHD-FMK or LEHD-CHO), and caspase-10 inhibitor (Z-AEVD-FMK) are used. These caspase inhibitors are dissolved in dimethyl sulfoxide (Me2SO); the final concentration of Me2SO is 0.1%. Cells (5×105) are preincubated in the presence or absence of 100 μM?each of these inhibitors for 3 h at 37°C then treated with or without 0.1, 0.5, and 1 μM?Paclitaxel for 48 h and processed for annexin V binding assay [1].

1×10^4 cells are plated in 100 μL of the growth medium in the presence or absence of increasing concentrations (0.1-1 μM) of taxol in 96-well plates and cultured at 37°C in 5% CO2 for 12-48 h. The cells are then incubated with 25 μL of MTT (5 mg/mL) at 37°C for 4 h. After dissolving the crystals with 0.04 N HCl in isopropanol, the plates are read in a microplate reader at 570 nm [1].

Adult (250-320 g) male Sprague-Dawley rats are used for all experiments. One week following the DiI injection, rats are anesthetized with isofluorane and injected into the tail vein with 2 mg/kg paclitaxel or its vehicle (1:1:23, cremophor EL:ethanol:0.9% saline). The tail vein injection is repeated three more times every other day for a total of four injections [4].

33069-62-4

C47H51NO14

853.918

Taxol;NSC 125973;紫杉醇

DMSO:85.4 mg/mL (100 mM)),with gentle warming
Ethanol:21.4 mg/mL (25 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years