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.
Cell Cycle. 2018;17(10):1235-1244.
Apatinib, a novel tyrosine kinase inhibitor, suppresses tumor growth in cervical cancer and synergizes with Paclitaxel.
Paclitaxel purchased from AbMole
Cancer Biol Ther. 2018 Feb 5.
Buformin suppresses proliferation and invasion via AMPK/S6 pathway in cervical cancer and synergizes with paclitaxel
Paclitaxel purchased from AbMole
|Source||Cell Cycle (2018 Jul). Figure 6. Paclitaxel (Abmole Bioscience)|
|Method||Tumor xenografts growth assay|
|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)|
|Cell Lines||MDA-MB-231 cells|
|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)|
|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|
|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|
|Cell Lines||PC-3 cells|
|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|
|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|
|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.|
|Incubation time||72 h|
|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|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO 80 mg/mL|
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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Crolibulin (also known as EPC2407 and crinobulin) is a small molecule tubulin polymerization inhibitor with potential antineoplastic activity.
Maytansinol, also known as Ansamitocin P-0, is a potent microtubule depolymerizing agent.
Epothilone D is a potent microtubule stabilizer.
|Estramustine phosphate sodium
Estramustine phosphate sodium is an antimicrotubule chemotherapy agent; arrests prostate cancer cells in the G2/M phase of the cell cycle.
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