Paclitaxel is a potent anticancer agent known to promote microtubule (MT) assembly, inhibit MT depolymerization, and change MT dynamics required for mitosis and cell proliferation.
Customer Validation
•Am J Cancer Res. 2017 Apr 1;7(4):903-912.
•Universidade do Porto. 2015-11-16.
•Universidade do Porto. Setembro/2015.
•Harvard Medical School LINCS LIBRARY
Description
Paclitaxel is a potent anticancer agent known to promote microtubule (MT) assembly, inhibit MT depolymerization, and change MT dynamics required for mitosis and cell proliferation.
IC50 & Target
IC50: 4 nM (MT)
In Vitro
Paclitaxel at 0.1, 0.5, and 1 μM reduces the proliferation and survival of CCRF-HSB-2 cells in a dose-dependent fashion and that the IC50 value of taxol is about 0.25 μM[1]. Paclitaxel directly associates with the endoplasmic reticulum to stimulate the release of calcium into the cytosol, contributing to the induction of apoptosis[2].
In Vivo
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]. Low doses of paclitaxel promot liver metastasis in mouse xenografts, which correlats with changes in estrogen metabolism in the host liver[4]. Paclitaxel (2 mg/kg per treatment, black circles) induces mechanical hypersensitivity in the glabrous skin of the hindpaw[5].
Clinical Trial
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References
[1]. Park SJ, et al. Taxol induces caspase-10-dependent apoptosis. J Biol Chem. 2004 Dec 3;279(49):51057-67. Epub 2004 Sep 27.
[2]. Pan Z, et al. Paclitaxel attenuates Bcl-2 resistance to apoptosis in breast cancer cells through an endoplasmic reticulum-mediated calciumrelease in a dosage dependent manner. Biochem Biophys Res Commun. 2013 Feb 13. pii: S0006-291X(13)00259-3.
[3]. Cadamuro M, et al. Low dose paclitaxel reduces S100A4 nuclear import to inhibit invasion and hematogenous metastasis of cholangiocarcinoma. Cancer Res. 2016 Jun 21.
[4]. Li Q, et al. Low doses of paclitaxel enhance liver metastasis of breast cancer cells in the mouse model. FEBS J. 2016 Jun 16.
[5]. Yilmaz E, et al. Sensory neuron subpopulation-specific dysregulation of intracellular calcium in a rat model of chemotherapy-induced peripheral neuropathy. Neuroscience. 2015 Aug 6;300:210-8.
[6]. Jing C, et al. Lenvatinib enhances the antitumor effects of paclitaxel in anaplastic thyroid cancer. Am J Cancer Res. 2017 Apr 1;7(4):903-912.
Preparing Stock Solutions
ConcentrationVolumeMass
1 mg
5 mg
10 mg
1 mM
1.1711 mL
5.8554 mL
11.7108 mL
5 mM
0.2342 mL
1.1711 mL
2.3422 mL
10 mM
0.1171 mL
0.5855 mL
1.1711 mL
Please refer to the solubility information to select the appropriate solvent.
Kinase Assay
[1]
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]
1×104 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. The concentration of drug that inhibits cell survival by 50% (IC50) is determined from cell survival plots. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[5]
Paclitaxel is dissolved at 25 mg/mL in 1:1 Cremophor EL: ethanol and freshly diluted 1:12.5 in 0.9% sterile saline prior to injections.
Adult (250-320 g) male Sprague-Dawley rats are used for all experiments. Rats are housed two per cage in a temperature and humidity controlled, on a 12 h:12 h light:dark schedule with food and water available ad libitum. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
[1]. Park SJ, et al. Taxol induces caspase-10-dependent apoptosis. J Biol Chem. 2004 Dec 3;279(49):51057-67. Epub 2004 Sep 27.
[2]. Pan Z, et al. Paclitaxel attenuates Bcl-2 resistance to apoptosis in breast cancer cells through an endoplasmic reticulum-mediated calciumrelease in a dosage dependent manner. Biochem Biophys Res Commun. 2013 Feb 13. pii: S0006-291X(13)00259-3.
[3]. Cadamuro M, et al. Low dose paclitaxel reduces S100A4 nuclear import to inhibit invasion and hematogenous metastasis of cholangiocarcinoma. Cancer Res. 2016 Jun 21.
[4]. Li Q, et al. Low doses of paclitaxel enhance liver metastasis of breast cancer cells in the mouse model. FEBS J. 2016 Jun 16.
[5]. Yilmaz E, et al. Sensory neuron subpopulation-specific dysregulation of intracellular calcium in a rat model of chemotherapy-induced peripheral neuropathy. Neuroscience. 2015 Aug 6;300:210-8.
[6]. Jing C, et al. Lenvatinib enhances the antitumor effects of paclitaxel in anaplastic thyroid cancer. Am J Cancer Res. 2017 Apr 1;7(4):903-912.
Molecular Weight
853.91
Formula
C₄₇H₅₁NO₁₄
CAS No.
33069-62-4
Storage
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
Shipping
Room temperature in continental US; may vary elsewhere
Solvent & Solubility
DMSO: ≥ 31 mg/mL; H2O: < 0.1="">
Paclitaxel is dissolved at 20 mg/mL in DMSO and freshly diluted (1:1-1:200) as a suspension with PBS.
Paclitaxel is dissolved in DMSO, aliquoted and stored at -80°C until further use. The same volume of DMSO is used as the vehicle control[6].
[1]. Park SJ, et al. Taxol induces caspase-10-dependent apoptosis. J Biol Chem. 2004 Dec 3;279(49):51057-67. Epub 2004 Sep 27.
[2]. Pan Z, et al. Paclitaxel attenuates Bcl-2 resistance to apoptosis in breast cancer cells through an endoplasmic reticulum-mediated calciumrelease in a dosage dependent manner. Biochem Biophys Res Commun. 2013 Feb 13. pii: S0006-291X(13)00259-3.
[3]. Cadamuro M, et al. Low dose paclitaxel reduces S100A4 nuclear import to inhibit invasion and hematogenous metastasis of cholangiocarcinoma. Cancer Res. 2016 Jun 21.
[4]. Li Q, et al. Low doses of paclitaxel enhance liver metastasis of breast cancer cells in the mouse model. FEBS J. 2016 Jun 16.
[5]. Yilmaz E, et al. Sensory neuron subpopulation-specific dysregulation of intracellular calcium in a rat model of chemotherapy-induced peripheral neuropathy. Neuroscience. 2015 Aug 6;300:210-8.
[6]. Jing C, et al. Lenvatinib enhances the antitumor effects of paclitaxel in anaplastic thyroid cancer. Am J Cancer Res. 2017 Apr 1;7(4):903-912.
Purity: 99.60%
Data Sheet (125 KB)SDS (556 KB)
COA (99 KB)HNMR (288 KB)LCMS (183 KB)
Handling Instructions (1252 KB)
[1]. Park SJ, et al. Taxol induces caspase-10-dependent apoptosis. J Biol Chem. 2004 Dec 3;279(49):51057-67. Epub 2004 Sep 27.
[2]. Pan Z, et al. Paclitaxel attenuates Bcl-2 resistance to apoptosis in breast cancer cells through an endoplasmic reticulum-mediated calciumrelease in a dosage dependent manner. Biochem Biophys Res Commun. 2013 Feb 13. pii: S0006-291X(13)00259-3.
[3]. Cadamuro M, et al. Low dose paclitaxel reduces S100A4 nuclear import to inhibit invasion and hematogenous metastasis of cholangiocarcinoma. Cancer Res. 2016 Jun 21.
[4]. Li Q, et al. Low doses of paclitaxel enhance liver metastasis of breast cancer cells in the mouse model. FEBS J. 2016 Jun 16.
[5]. Yilmaz E, et al. Sensory neuron subpopulation-specific dysregulation of intracellular calcium in a rat model of chemotherapy-induced peripheral neuropathy. Neuroscience. 2015 Aug 6;300:210-8.
[6]. Jing C, et al. Lenvatinib enhances the antitumor effects of paclitaxel in anaplastic thyroid cancer. Am J Cancer Res. 2017 Apr 1;7(4):903-912.