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Paclitaxel

Cat. No. M1970
Paclitaxel Structure
Synonym:

Taxol

Size Price Availability Quantity
50mg USD 60 In stock
100mg USD 90 In stock
500mg USD 150 In stock
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Quality Control
Biological Activity

Paclitaxel (Taxol) is a potent anti-neoplastic and anti-mitotic taxane compound used in cancer chemotherapy. Paclitaxel binds to the N-terminus of β-tubulin and and stabilizes microtubules arresting the cell cycle at the G2/M phase. The microtubule damage induces apoptosis through a JNK-dependent pathway followed by a JNK-independent pathway, perhaps related to the activation of protein kinase A (PKA) or of Raf-1 kinase, resulting in phosphorylation of Bcl-2. Paclitaxel stabilizes microtubules and as a result, interferes with the normal breakdown of microtubules during cell division. The ability of paclitaxel to inhibit spindle function is generally attributed to its suppression of microtubule dynamics, but recent studies have demonstrated that suppression of dynamics occurs at concentrations lower than those needed to block mitosis. At the higher therapeutic concentrations, paclitaxel appears to suppress microtubule detachment from centrosomes, a process normally activated during mitosis. The binding site for paclitaxel has been identified on the beta-tubulin subunit. In vitro and in vivo studies have demonstrated that paclitaxel is extensively metabolised by the liver to 3 primary metabolites.

Protocol
Cell Experiment
Cell lines human neonatal dermal microvascular ECs (HMVECs), human umbilical vein ECs (HUVECs), human umbilical artery ECs (HUAVECs), normal human astrocytes (NHAs), normal human dermal fibroblasts (NHDFs), normal human epidermal keratinocytes (NHEKs
Preparation method Cells including human neonatal dermal microvascular ECs (HMVECs), human umbilical vein ECs (HUVECs), human umbilical artery ECs (HUAVECs), normal human astrocytes (NHAs), normal human dermal fibroblasts (NHDFs), normal human epidermal keratinocytes (NHEKs), human mammary epithelial cells (HMEpCs), human prostate epithelial cells (PrEpCs) and human umbilical artery smooth muscle cells (UASMCs) are cultured. Cell proliferations are performed in 96-well plates using cells between passages 6 and 12. Cells are seeded at 3000–5000 cells/well and allowed to attach for 4 hours. Paclitaxel, diluted in culture medium, is added in quadruplicate wells and the cells ae incubated for 3 days before MTS reagents are added to quantitate the live cells in each well.
Concentrations 0.1-100 pM
Incubation time 72 h
Animal Experiment
Animal models nude athymic mice with BC-V and BC-ER tumors
Formulation Dissolved in absolute ethanol with an equal volume of cremophor and diluted 1:4 with sterile physiological saline before use
Dosages 20 mg/kg
Administration i.v.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 853.91
Formula C47H51NO14
CAS Number 33069-62-4
Purity 99.31%
Solubility DMSO 80 mg/mL
Storage at -20°C
References

Enhanced oral paclitaxel bioavailability after administration of paclitaxel-loaded lipid nanocapsules.
Peltier S, et al. Pharm Res. 2006 Jun;23(6):1243-50. PMID: 16715372.

Cytotoxic studies of paclitaxel (Taxol) in human tumour cell lines.
Liebmann JE, et al. Br J Cancer. 1993 Dec;68(6):1104-9. PMID: 7903152.

Clinical pharmacokinetics of paclitaxel.
Sonnichsen DS, et al. Clin Pharmacokinet. 1994 Oct;27(4):256-69. PMID: 7834963.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Paclitaxel, Taxol supplier, Microtubule, inhibitors

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