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Paclitaxel

Cat. No. M1970
Paclitaxel Structure
Synonym:

Taxol; NSC 125973

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 40  USD40 In stock
10mg USD 25  USD25 In stock
50mg USD 40  USD40 In stock
100mg USD 80  USD80 In stock
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Quality Control & Documentation
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.

Product Citations
Customer Product Validations & Biological Datas
Source Cell Cycle (2018 Jul). Figure 6. Paclitaxel (Abmole Bioscience)
Method Tumor xenografts growth assay
Cell Lines mice
Concentrations 150 mg/kg/day
Incubation Time days 1 to 14
Results Apatinib or Paclitaxel significantly suppressed the growth of SiHa xenografts, and the combination with the 2 drugs further augmented this effect
Source Customer experimental result (2018 Aug). Figure 1. Paclitaxel (Abmole)
Method apoptosis assay
Cell Lines MDA-MB-231 cells
Concentrations 2μM
Incubation Time 24 hours
Results MDA-MB-231 cells were treated by paclitaxel (2μM) for 24 hours, obvious apoptosis was observed compared with the negative group.
Source Cancer Biol Ther (2018). Figure 7. Paclitaxel (Abmole Bioscience, Shanghai, China)
Method intraperitoneal injection
Cell Lines female Balb/c nude mice
Concentrations 15 mg/kg/twice a week
Incubation Time 10 days
Results As the growth curve demonstrates, compared to the control group, tumor growth was significantly suppressed in both the buformin and paclitaxel groups.
Source Cancer Biol Ther (2018). Figure 6. Paclitaxel (Abmole Bioscience, Shanghai, China)
Method Buformin synergizes with chemotherapy
Cell Lines C33A cells
Concentrations 1 μM
Incubation Time
Results In C33A cells, low-dose buformin (1μM) significantly enhanced the anti-proliferative effects when combined with cisplatin, paclitaxel, or 5-FU
Source J Control Release (2015). Figure 7. Paclitaxel
Method Viability assays
Cell Lines PC-3 cells
Concentrations 5 μM
Incubation Time 24 h
Results PtX from the medium caused the cells to eventually lose their elongated, branched shape and become spherical before they started dissociating and dying.
Source J Control Release (2015). Figure 5. Paclitaxel
Method Measurement of EV-bound Paclitaxel
Cell Lines PCa cells
Concentrations 5 μM
Incubation Time 24 and 48 h
Results The cytotoxic effect of the PtX-EVs on autologous PCa cells was compared to the free drug by viability assays. Cell viability curves were established as a function of PtX-EV dose for both PC-3 and LNCaP cells
Protocol (for reference only)
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.
Chemical Information
Molecular Weight 853.91
Formula C47H51NO14
CAS Number 33069-62-4
Solubility (25°C) DMSO 50 mg/mL
Storage -20°C, protect from light, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Peltier S, et al. Pharm Res. Enhanced oral paclitaxel bioavailability after administration of paclitaxel-loaded lipid nanocapsules.

[2] Liebmann JE, et al. Br J Cancer. Cytotoxic studies of paclitaxel (Taxol) in human tumour cell lines.

[3] Sonnichsen DS, et al. Clin Pharmacokinet. Clinical pharmacokinetics of paclitaxel.

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Keywords: Paclitaxel, Taxol; NSC 125973 supplier, Microtubule, inhibitors, activators


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