Cabazitaxel-XRP6258-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECabazitaxelCat. No.: HY-15459CAS No.: 183133-96-2Synonyms: XRP6258; RPR-116258A; taxoid XRP6258分式: CHNO分量: 835.93作靶點: Microtubule/Tubulin; Autophagy作通路: Cell Cycle/DNA Damage; Cytoskeleton; Autophagy儲存式: Powder -20C 3 years4C 2

2、yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 100 mg/mL (119.63 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.1963 mL 5.9814 mL 11.9627 mL5 mM 0.2393 mL 1.1963 mL 2.3925 mL10 mM 0.1196 mL 0.5981 mL 1.1963 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請

3、注意儲備液的保存式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (2.99 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubili

4、ty: 2.5 mg/mL (2.99 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (2.99 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Cabazitaxel天然紫杉烷脫酰 巴卡丁III的半合成衍物，具有顯著的抗腫瘤功效。體外研究 The cytotoxicity of cabazitaxel (100 g/mL) on 4T1 cells wit

5、hout irradiation is 70.8%. Cabazitaxel (100 g/mL)exhibits a concentration-dependent antiproliferation effect, with the antiproliferative activity of 56.2% 1.體內(nèi)研究 Cabazitaxel (10 mg/kg, i.v.) has certain toxicity to liver and kidney but it can be avoided by integrated intoAns. The body weights of mic

6、e treated with AN-ICG-CBX and AN-CBX have a slightly decrease, while bodyweights of the free CBX group significantly decrease compared to the control group 1.PROTOCOLCell Assay 1 The cytotoxicity of CBX-loaded ANs and free Cabazitaxel (CBX) is evaluated with MTT assay. Cells areseeded onto a 96-well

7、 plate at a density of 3000 cells per well and cultured for 24 h. CBX-loaded ANs andfree CBX are diluted to predetermined concentrations with PBS and added into each well. Blank AN, AN-ICGand free CBX solvent (a mixture of Tween-80 and anhydrous alcohol) are added as well to different finalconcentra

8、tions. The incubation continued for another 48 hours. 20 L MTT solutions (5 mg/mL in PBS) areadded into each well and cells are incubated for another 4 hours under 37C. Subsequently the medium isremoved and 150 L dimethyl sulphoxide (DMSO) is added to dissolve the purple formazan salt crystals.Then

9、the absorbance is measured by a microplate reader at 490 nm. The cells treated with medium areevaluated as controls.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal To evaluate the antitumor efficiency of the combined chemotherapy and PTT in vivo,

10、 mice bearing 4T1 tumorAdministration 1 are randomLy divided into 6 treatment groups (n=5). Treatment begin when the tumors reached 50 mm3-100mm3. The mice are intravenously injected with saline, AN-ICG, free Cabazitaxel (CBX), AN-CBX and AN-ICG-CBX (ICG 2 mg/kg, CBX 10 mg/kg). 8 hours later, the gr

11、oups injected with AN-ICG and AN-ICG-CBX isirradiated by the 808 nm laser (0.8 W/cm2, 5 min). The length and width of every tumor are measured by acaliper every other day. The formula (volume (mm3) =1/2 length width2) is used to calculate the tumorvolume. The body weights of these mice are recorded

12、every two days using an electronic balance as well. Atthe end of the antitumor study, the 4T1 tumor bearing mice are sacrificed to collect the tumors and majororgans.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 Nanomedicine (Lond). 2017 S

13、ep;12(17):2083-2095. Chin J Cancer. 2015 Mar 5;34(3):115-20.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE Prostate. 2018 Sep;78(12):905-914. Prostate. 2018 Feb;78(3):166-177. Methods Mol Biol. 2018;1711:351-398.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Tai X, et al. C

14、abazitaxel and indocyanine green co-delivery tumor-targeting nanoparticle for improved antitumor efficacy and minimizeddrug toxicity. J Drug Target. 2016 Sep 9:1-29.2. Gdowski AS, et al. Bone-targeted cabazitaxel nanoparticles for metastatic prostate cancer skeletal lesions and pain. Nanomedicine(Lond). 2017 Sep;12(17):