Cabazitaxel
Catalog No.S3022 Synonyms: RPR-116258A, XRP6258, TXD 258
Molecular Weight(MW): 835.93
Cabazitaxel is a semi-synthetic derivative of a natural taxoid that kills cancer cells by inhibiting cell division and growth. Cabazitaxel exerts its effects by inhibiting microtubule growth and assembly, processes that are essential for cells to divide.
3 Customer Reviews
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ABCB1 functional inhibition using elacridar re-sensitizes TaxR and DU145-DTXR cells to cabazitaxel treatment. A. TaxR and DU145-DTXR cells were subjected to cell growth assays using either vehicle (DMSO), elacridar (0.5μM), cabazitaxel (1nM), or a combination of elacridar and cabazitaxel. Cells were counted 72 hours post-treatment. B. TaxR and DU145-DTXR cells were treated with either vehicle (DMSO), elacridar (0.5μM), cabazitaxel (1nM), or a combination of both elacridar and cabazitaxel for 72 hours. Whole cell lysates were then prepared and subjected to western blot analysis using indicated antibodies. Tubulin served as a loading control. c-PARP = cleaved-PARP, C = control (DMSO) treatment, Elac = elacridar, CTX = cabazitaxel. All data is presented as percent of control mean ± standard deviation. * = p-value ≤ 0.05.
Mol Cancer Ther, 2017, 16(10):2257-2266. Cabazitaxel purchased from Selleck.
Combination effect of cabazitaxel with drugs that target the PI3K-pathway simultaneously: LNCaP cells were treated with the indicated combination of the drugs and analyzed as described in Methods and Figure Figure3
Oncotarget, 2016, 7(46):76181-76196. Cabazitaxel purchased from Selleck.
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Viability of PC-3R and PC-3 cells treated with docetaxel and cabazitaxel. The 3,000 cells seeded in a 96-well plate were treated with docetaxel or cabazitaxel at indicated concentrations for 72 hours and subjected to WST assay (n=5).
Urol Oncol, 2015, 33(9):385.e15-20.. Cabazitaxel purchased from Selleck.
Purity & Quality Control
Choose Selective Microtubule Associated Inhibitors
Biological Activity
| Description | Cabazitaxel is a semi-synthetic derivative of a natural taxoid that kills cancer cells by inhibiting cell division and growth. Cabazitaxel exerts its effects by inhibiting microtubule growth and assembly, processes that are essential for cells to divide. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Features | A semi-synthetic derivative of a natural taxoid. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Targets |
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| In vitro |
Cabazitaxel increases CYP3A enzyme activities in rat hepatocytes. The mean ex-vivo human plasma protein binding of Cabazitaxel is 91.6%. Cabazitaxel is rapidly and extensively metabolised in numerous metabolites. Cabazitaxel demonstrates activity in several murine and human resistant cell lines. [1] With a 4-day exposure to cabazitaxel, cytotoxicity is noted with relatively low cabazitaxel concentrations. Cabazitaxel shows high antitumor activity in 3 human colorectal cell lines (HCT-116, HCT-8, and HT-29). [2] |
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| Cell Data |
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| In vivo | In accompanying models, Cabazitaxel is noted to have significant antitumor activity. In murine tumor xenografts (colon C38 and pancreas P03), Cabazitaxel elicites complete tumor regressions. Using SF-295 and U251 human glioblastoma cell lines, both orthotopic and subcutaneous murine xenografts are generated. Cabazitaxel treatment leads to complete regression in the majority of subcutaneously implanted tumors. Furthermore, in orthotopic models, Cabazitaxel leads to complete tumor regression in 4 out of 10 U251 tumors. [2] |
Protocol
Solubility (25°C)
| In vitro | DMSO | 100 mg/mL (119.62 mM) |
|---|---|---|
| Water | Insoluble | |
| Ethanol | Insoluble |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 835.93 |
|---|---|
| Formula | C45H57NO14 |
| CAS No. | 183133-96-2 |
| Storage | powder |
| in solvent | |
| Synonyms | RPR-116258A, XRP6258, TXD 258 |
Bio Calculators
Molarity Calculator
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03110588 | Recruiting | Metastatic Prostate Cancer | University of Alabama at Birmingham|Astellas Pharma Inc|Sanofi | July 1 2018 | Phase 1 |
| NCT03419234 | Recruiting | Castration Levels of Testosterone|Castration-Resistant Prostate Carcinoma|Metastatic Prostate Carcinoma in the Soft Tissue|Prostate Carcinoma Metastatic in the Bone|Stage IV Prostate Adenocarcinoma AJCC v7 | ECOG-ACRIN Cancer Research Group|National Cancer Institute (NCI)|Eastern Cooperative Oncology Group | February 8 2018 | Phase 2 |
| NCT03257891 | Recruiting | Adrenocortical Carcinoma | Azienda Ospedaliera Spedali Civili di Brescia|San Luigi Gonzaga Hospital | January 25 2018 | Phase 2 |
| NCT03392428 | Recruiting | Cancer of the Prostate|Metastatic Cancer | Australian and New Zealand Urogenital and Prostate Cancer Trials Group|Australian Nuclear Science and Technology Organisation (ANSTO)|Endocyte|Prostate Cancer Foundation of Australia (PCFA)|Australasian Radiopharmaceutical Trials network (ARTnet)|Movember Foundation | January 29 2018 | Phase 2 |
| NCT02844582 | Recruiting | Hormone-Resistant Prostate Cancer|Stage IV Prostate Adenocarcinoma | University of California Davis|Sanofi | December 20 2017 | Phase 2 |
| NCT03356912 | Enrolling by invitation | Prostate Cancer|Castration-resistant Prostate Cancer | Consorzio Oncotech | November 22 2017 | Phase 2 |
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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Frequently Asked Questions
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Question 1:
What is the elimination half-life of cabazitaxel?
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Answer:
According to the paper report, the elimination half-life of cabazitaxel is 95h.
