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.
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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|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.|
|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)|
* 1 mg/ml means slightly soluble or 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.
|Synonyms||RPR-116258A, XRP6258, TXD 258|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02961257||Not yet recruiting||Prostate Cancer Metastatic||Association Pour La Recherche des Thérapeutiques Innovantes en Cancérologie||March 2017||Phase 3|
|NCT03050866||Not yet recruiting||Circulating Tumor Cell|Metastatic Prostate Cancer||Erasmus Medical Center|Sanofi||February 2017||Phase 2|
|NCT02903160||Not yet recruiting||Prostate Cancer||Icahn School of Medicine at Mount Sinai|Sanofi|Bayer||October 2016||Phase 2|
|NCT02844582||Not yet recruiting||Hormone-Resistant Prostate Cancer|Stage IV Prostate Adenocarcinoma||University of California, Davis|Sanofi||October 2016||Phase 2|
|NCT02543255||Recruiting||Prostate Cancer||University Health Network, Toronto||September 2016||Phase 2|
|NCT02703623||Recruiting||Prostate Cancer||M.D. Anderson Cancer Center|Bristol-Myers Squibb|Janssen, LP|Sanofi||May 2016||Phase 2|
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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