product name Paclitaxel
Description: Paclitaxel (also known as NSC 125973) is a highly potent microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells. It is a natural product isolated from the Pacific yew tree Taxus brevifolia that has anticancer activity. Paclitaxel binds to tubulin and inhibits the disassembly of microtubules, thereby resulting in the inhibition of cell division. This agent also induces apoptosis by binding to and blocking the function of the apoptosis inhibitor protein Bcl-2.
References: Anticancer Drugs. 2003 Jan;14(1):13-9; Breast Cancer Res Treat. 2012 Aug;134(3):969-80.
853.91
Formula
C47H51NO14
CAS No.
33069-62-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 171 mg/mL (200.3 mM)
Water: <1 mg/mL
Ethanol: 18 mg/mL (21.1 mM)
Solubility (In vivo)
1% DMSO+30% polyethylene glycol+1% Tween 80: 30 mg/mL
Synonyms
NSC 125973
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19396667
| In Vitro |
In vitro activity: Paclitaxel inhibits non-endothelial type human cells at 104 – to 105 -fold higher concentrations, with IC50 of 1 nM-10 nM. The selectivity of Paclitaxel inhibition of cell proliferation is also species specific, as mouse ECs are not sensitive to Paclitaxel at ultra low concentrations. Inhibition of human ECs by Paclitaxel at ultra low concentrations does not affect the cellular microtubule structure, and the treated cells do not show G2/M cell cycle arrest and apoptosis, suggesting a novel but as yet unidentified mechanism of action. In an in vitro angiogenesis assay, Paclitaxel at ultra low concentrations blocks human ECs from forming sprouts and tubes in the three-dimensional fibrin matrix. In the presence of SMF, the efficient concentration of Paclitaxel on K562 cells is decreased from 50 to 10 ng/mL. The cell cycle arrest effect of Paclitaxel with or without SMF on K562 cells is correlated with DNA damage. Paclitaxel alone causes a time-dependent inhibition of CDK1 in four cell lines including A549 cells, H358, H1395 cells and H1666 cells. Kinase Assay: Cell Assay: 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. |
|---|---|
| In Vivo | The inhibition rations of Paclitaxel alone on BC-V and BC-ER tumors are 49.78% and 51.23%, respectively. Treatment of six cycles of 20 mg/kg Paclitaxel significantly reduces the percentages of Ki-67-positive cells to 20.4% in BC-V tumors and 25.1% in BC-ER tumors, respectively. |
| Animal model | Female, 20-22 g homozygous nude athymic mice with BC-V and BC-ER tumors |
| Formulation & Dosage | Dissolved in absolute ethanol with an equal volume of cremophor and diluted 1:4 with sterile physiological saline before use.; 20 mg/kg; i.v. injection |
| References | Anticancer Drugs. 2003 Jan;14(1):13-9; Breast Cancer Res Treat. 2012 Aug;134(3):969-80. |
Related Posts
product name Paclitaxel
Description: Paclitaxel (also known as NSC 125973) is a highly potent microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells. It is a natural product isolated from the Pacific yew tree Taxus brevifolia that has anticancer activity. Paclitaxel binds to tubulin and inhibits the disassembly of microtubules, thereby resulting in the inhibition of cell division. This agent also induces apoptosis by binding to and blocking the function of the apoptosis inhibitor protein Bcl-2.
References: Anticancer Drugs. 2003 Jan;14(1):13-9; Breast Cancer Res Treat. 2012 Aug;134(3):969-80.
853.91
Formula
C47H51NO14
CAS No.
33069-62-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 171 mg/mL (200.3 mM)
Water: <1 mg/mL
Ethanol: 18 mg/mL (21.1 mM)
Solubility (In vivo)
1% DMSO+30% polyethylene glycol+1% Tween 80: 30 mg/mL
Synonyms
NSC 125973
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19396667
| In Vitro |
In vitro activity: Paclitaxel inhibits non-endothelial type human cells at 104 – to 105 -fold higher concentrations, with IC50 of 1 nM-10 nM. The selectivity of Paclitaxel inhibition of cell proliferation is also species specific, as mouse ECs are not sensitive to Paclitaxel at ultra low concentrations. Inhibition of human ECs by Paclitaxel at ultra low concentrations does not affect the cellular microtubule structure, and the treated cells do not show G2/M cell cycle arrest and apoptosis, suggesting a novel but as yet unidentified mechanism of action. In an in vitro angiogenesis assay, Paclitaxel at ultra low concentrations blocks human ECs from forming sprouts and tubes in the three-dimensional fibrin matrix. In the presence of SMF, the efficient concentration of Paclitaxel on K562 cells is decreased from 50 to 10 ng/mL. The cell cycle arrest effect of Paclitaxel with or without SMF on K562 cells is correlated with DNA damage. Paclitaxel alone causes a time-dependent inhibition of CDK1 in four cell lines including A549 cells, H358, H1395 cells and H1666 cells. Kinase Assay: Cell Assay: 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. |
|---|---|
| In Vivo | The inhibition rations of Paclitaxel alone on BC-V and BC-ER tumors are 49.78% and 51.23%, respectively. Treatment of six cycles of 20 mg/kg Paclitaxel significantly reduces the percentages of Ki-67-positive cells to 20.4% in BC-V tumors and 25.1% in BC-ER tumors, respectively. |
| Animal model | Female, 20-22 g homozygous nude athymic mice with BC-V and BC-ER tumors |
| Formulation & Dosage | Dissolved in absolute ethanol with an equal volume of cremophor and diluted 1:4 with sterile physiological saline before use.; 20 mg/kg; i.v. injection |
| References | Anticancer Drugs. 2003 Jan;14(1):13-9; Breast Cancer Res Treat. 2012 Aug;134(3):969-80. |