For research use only.
Catalog No.S3022 Synonyms: RPR-116258A, XRP6258, TXD 258, Taxoid XRP6258
CAS No. 183133-96-2
Cabazitaxel (RPR-116258A, XRP6258, TXD 258, Taxoid XRP6258) 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. Cabazitaxel induces autophagy via the PI3K/Akt/mTOR pathway.
Selleck's Cabazitaxel has been cited by 19 publications
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|Description||Cabazitaxel (RPR-116258A, XRP6258, TXD 258, Taxoid XRP6258) 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. Cabazitaxel induces autophagy via the PI3K/Akt/mTOR pathway.|
|Features||A semi-synthetic derivative of a natural taxoid.|
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.  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). 
|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. |
|In vitro||DMSO||100 mg/mL (119.62 mM)|
* 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.
|Synonyms||RPR-116258A, XRP6258, TXD 258, Taxoid XRP6258|
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04622761||Not yet recruiting||Drug: Cabazitaxel||Prostate Cancer||The Clatterbridge Cancer Centre NHS Foundation Trust|University of Liverpool||November 12 2020||Phase 2|
|NCT04495179||Recruiting||Drug: AZD4635|Drug: Durvalumab|Drug: Cabazitaxel||Progressive Metastatic Castrate-Resistant Prostate Cancer||AstraZeneca|Parexel||August 4 2020||Phase 2|
|NCT03257891||Recruiting||Drug: Cabazitaxel||Adrenocortical Carcinoma||Azienda Socio Sanitaria Territoriale degli Spedali Civili di Brescia|San Luigi Gonzaga Hospital||January 25 2018||Phase 2|
|NCT02844582||Completed||Drug: Cabazitaxel|Drug: Prednisone||Hormone-Resistant Prostate Cancer|Stage IV Prostate Adenocarcinoma||University of California Davis|Sanofi||December 20 2017||Phase 2|
|NCT03043989||Terminated||Drug: Docetaxel|Drug: Cabazitaxel|Drug: Clarithromycin||Prostate Cancer||Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Maryland Technology Development Corporation||March 21 2017||Phase 1|
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
What is the elimination half-life of cabazitaxel?
According to the paper report, the elimination half-life of cabazitaxel is 95h.