Cabazitaxel

Manufactured by MedChemExpress

Sourced in United States

Cabazitaxel is a microtubule inhibitor that binds to tubulin, disrupting the microtubule network within cells. This ultimately leads to cell cycle arrest and apoptosis. Cabazitaxel is commonly used as a research tool in the study of cell biology and cancer research.

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4 protocols using cabazitaxel

Evaluating Cell Viability and Sensitivity

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We performed a CCK-8 assay (Cellcook, Guangzhou, China, Cat No. CT01A) using the manufacturer’s guidelines to determine the viability of cells transfected with DDIT4-siRNA and siRNA-NC. We seeded these cells in the logarithmic growth phase into 96-well plates. In order to evaluate the effect on cell proliferation capacity, 10 μl CCK-8 reagent was added in all wells and incubated for 2 hours at 37°C at 0, 24, 48, 72 h after culturing. For the sensitivity of cells to the drug, cells were treated at 37˚C with Ispinesib (0, 20, 40, 80 or 100 nM, MedChem Express, Monmouth Junction, NJ, USA, Cat No.HY-50759), Cabazitaxel (0, 10, 20, 40 or 80 nM, MedChem Express, Monmouth Junction, NJ, USA, Cat No. HY-15459) and Epothilone-b (0, 40, 80, 160 or 320 nM, MedChem Express, Monmouth Junction, NJ, USA, Cat No. HY-17029) for 24 h, respectively. 10 μl CCK-8 reagent was added in all wells and incubated for 2 hours at 37°C. Finally, we measured the absorbance of each well at 450 nm using a microplate reader.

Zhang Y., Wang Y., Chen J., Xia Y, & Huang Y. (2023). A programmed cell death-related model based on machine learning for predicting prognosis and immunotherapy responses in patients with lung adenocarcinoma. Frontiers in Immunology, 14, 1183230.

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Preparation and Characterization of Cyclodextrin Nanoparticles

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Cabazitaxel (CBX, purity 99.92%, CAS 183133-96-2) and bicalutamide, (BIC, racemic mixture, purity 99.85%, CAS 90357-06-5) were purchased from MedChemExpress; chlorin e6 sc-263067 (purity > 95%, Santa Cruz Biotechnology, Inc.) was purchased from Santa Cruz Biotechnology, Inc. The polymers were produced by crosslinking CyD monomers under strongly alkaline conditions in the presence of epichlorohydrin (EPI). The pβCyD NPs, were recovered by ultrafiltration followed by freeze-drying. ¹H NMR spectroscopy was used to determine the CyD content. The polymers contain 60–70% w/w of CyD, have a molecular weight of 50–60 kDa determined by means of size exclusion chromatography. DLS with a Malvern Nanosizer system was used to determine the particle size of the loaded polymers and to check on possible aggregation over time. All solvents were of analytic or spectroscopic grade.

Pancani E., Veclani D., Agnes M., Mazza A., Venturini A., Malanga M, & Manet I. (2023). Three-in-one: exploration of co-encapsulation of cabazitaxel, bicalutamide and chlorin e6 in new mixed cyclodextrin-crosslinked polymers. RSC Advances, 13(16), 10923-10939.

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Formulation and Characterization of Cabazitaxel-Loaded PLGA Nanoparticles

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The nanoparticles were prepared using a water-in-oil-in-water emulsion solvent evaporation similar to that described previously [11 (link)]. Briefly, 20 mg/ml PLGA 50:50 iv. 0.77 dl/g (∼0.5% w/v in chloroform at 30°C); 124 kDa mw (Lakeshore Biomaterials) and 5% cabazitaxel (MedChem Express, NJ, USA) was dissolved in 2 ml ethyl acetate. 400 μl of phosphate-buffered saline (PBS) was added to the 2 ml ethyl acetate PLGA solution and vortexed for 30 s, followed by sonicating with ultrasonic processor UP200H system (Hielscher Ultrasonics GmbH, Germany) twice at 40% amplitude for 30 s on ice. This mixture was then transferred to an aqueous solution of 10 ml of 1% poly (vinyl-alcohol) (Sigma) plus 0.5 mg/ml of (Bis[sulfosuccinimidyl] suberate (BS3) crosslinker (ProteoChem) followed by sonication for 1 min on pulsing mode at 40% amplitude on ice. Excess solvent was evaporated under continuous magnetic stirring for 2–3 h. These nanoparticles were washed three-times by centrifugation and resuspended in water. Nanoparticles were then lyophilized on ATR FD 3.0 system (ATR Inc., MO, USA) and stored at 4°C until used.

Gdowski A.S., Ranjan A., Sarker M.R, & Vishwanatha J.K. (2017). Bone-targeted cabazitaxel nanoparticles for metastatic prostate cancer skeletal lesions and pain. Nanomedicine, 12(17), 2083-2095.

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Screening Spectrum Collection Compounds for OATP1B1 Inhibition

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Compounds from the Spectrum Collection, distributed in 80 wells of 96 well plates (100 nmol per well in 10 μl of DMSO), were screened for their inhibitory effectiveness against transport of E3S into CHO cells expressing OATP1B1; a total of 560 compounds were used. Each compound was diluted to a concentration of 20 μM, pH 7.4, to a final concentration of 2% dimethylsulfoxide (DMSO) using a VIAFLO multichannel electronic pipet (Integra Biosciences, Hudson, NH) ⁶⁵. The following compounds for prospective testing were purchased from MedChemExpress (Monmouth Junction, NJ): abamectin, asiaticoside, baloxavir, berbamine, bremelanotide, bromocriptine, cabazitaxel, doramectin, etoposide, lapatinib, mobocertinib, novobiocin, posaconazole, rifaximin, teniposide, umbralisib, vancomycin, vinblastine and vincristine. Pyronaridine tetraphosphate was purchased from BOC Sciences (Shirley, NY) and tilorone hydrochloride from Caymen Chemical Company (Ann Arbor, MI). These compounds were solubilized in DMSO at 20 mM prior to tested.

Lane T.R., Urbina F., Zhang X., Fye M., Gerlach J., Wright S.H, & Ekins S. (2022). Machine Learning Models Identify New Inhibitors for Human OATP1B1. Molecular pharmaceutics, 19(11), 4320-4332.

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