1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPaclitaxelCat. No.: HY-B0015CAS No.: 33069-62-4Synonyms: Taxol分式: CHNO分量: 853.91作靶點: Microtubule/Tubulin; ADC Cytotoxin; Autophagy作通路: Cell Cycle/DNA Damage; Cytoskeleton; Antibody-drugConjugate/ADC Related; Autophagy儲存式: 4C, pr

2、otect from light* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性數據體外實驗 DMSO : 31 mg/mL (36.30 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (2.93 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% corn oil1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.

3、5 mg/mL (2.93 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Paclitaxel (Taxol)種天然的抗癌藥物，能穩(wěn)定微管蛋聚合，并導致細胞周 期的 G2/M 期停滯和凋亡細胞死亡 1 2。IC50 & Target IC50: 4 nM (Microtubule)體外研究 Paclitaxel (20 nM; 48 hours) induces programmed cell death and exists a block at the G2/M phase of the cellcycle 1.Paclitaxel (20 nM; 4

4、8 hours) induces a consistent increase in the level of p53 1.Apoptosis Analysis 1Cell Line: MCF-7, MDA-MB-231 cellsConcentration: 20 nMIncubation Time: 48 hoursResult: Induced programmed cell death.Cell Cycle Analysis 1Cell Line: MCF-7, MDA-MB-231 cellsConcentration: 20 nMIncubation Time: 48 hoursRe

5、sult: 60% of MCF-7 cells and 50% of MDA-MB-231 cells were in the G2/M phase following24 h treament.Western Blot Analysis 1Cell Line: MCF-7 cells (harboring wild-type p53)Concentration: 20 nMIncubation Time: 48 hoursResult: Induced a consistent increase in the level of p53.體內研究Paclitaxel (1-20 mg/kg;

6、 i.p.; 1 time/2 days for five cycles) obviously induces liver metastases at the low-Paclitaxel group with little influence on primary tumor growth 3.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEAnimal Model: MDA-231 xenograft-bearing mice 3Dosage: 1, 20 mg/kgAdministration: Intraperitoneal injec

7、tion; five cycles (1 time/2 days)Result: Liver metastases were obviously induced in the low-PTX (1 mg/kg) group with littleinfluence on primary tumor growth compared with high-PTX group.戶使本產品發(fā)表的科研獻 Cell Syst. 2019 Jul 5. pii: S2405-4712(19)30200-5. J Control Release. 2018 May 10;277:23-34. Thyroid.

8、2019 Jun;29(6):809-823. Cell Mol Immunol. 2019 Jun 3. FASEB J. 2019 Apr;33(4):5520-5534.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Choi YH, et al. Taxol-induced growth arrest and apoptosis is associated with the upregulation of the Cdk inhibitor, p21WAF1/CIP1, inhuman brea

9、st cancer cells. Oncol Rep. 2012 Dec;28(6):2163-9.2. Dziadyk JM, et al. Paclitaxel-induced apoptosis may occur without a prior G2/M-phase arrest. Anticancer Res. 2004 Jan-Feb;24(1):27-36.3. Li Q, et al. Low doses of paclitaxel enhance liver metastasis of breast cancer cells in the mouse model. FEBS

10、J. 2016Aug;283(15):2836-52.4. Pan Z, et al. Paclitaxel attenuates Bcl-2 resistance to apoptosis in breast cancer cells through an endoplasmic reticulum-mediatedcalciumrelease in a dosage dependent manner. Biochem Biophys Res Commun. 2013 Feb 13. pii: S0006-291X(13)00259-3.5. Cadamuro M, et al. Low d

11、ose paclitaxel reduces S100A4 nuclear import to inhibit invasion and hematogenous metastasis ofcholangiocarcinoma. Cancer Res. 2016 Jun 21.6. Li Q, et al. Low doses of paclitaxel enhance liver metastasis of breast cancer cells in the mouse model. FEBS J. 2016 Jun 16.7. Yilmaz E, et al. Sensory neuro

12、n subpopulation-specific dysregulation of intracellular calcium in a rat model of chemotherapy-inducedperipheral neuropathy. Neuroscience. 2015 Aug 6;300:210-8.8. Jing C, et al. Lenvatinib enhances the antitumor effects of paclitaxel in anaplastic thyroid cancer. Am J Cancer Res. 2017 Apr1;7(4):903-912.McePdfHeightCaution: P