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Cabazitaxel (Synonyms: XRP6258; RPR-116258A; taxoid XRP6258)

Cat. No.: HY-15459 Purity: 99.89%
Data Sheet SDS Handling Instructions

Cabazitaxel is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity.

For research use only. We do not sell to patients.
Cabazitaxel Chemical Structure

Cabazitaxel Chemical Structure

CAS No. : 183133-96-2

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Description

Cabazitaxel is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity.

In Vitro

The cytotoxicity of cabazitaxel (100 μg/mL) on 4T1 cells without irradiation is 70.8%. Cabazitaxel (100 μg/mL) exhibits a concentration-dependent antiproliferation effect, with the antiproliferative activity of 56.2%[1].

In Vivo

Cabazitaxel (10 mg/kg, i.v.) has certain toxicity to liver and kidney but it can be avoided by integrated into Ans. The body weights of mice treated with AN-ICG-CBX and AN-CBX have a slightly decrease, while body weights of the free CBX group significantly decrease compared to the control group[1].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01518283 Spanish Oncology Genito-Urinary Group Hormone Refractory Prostate Cancer May 2012 Phase 2
NCT02512458 Hellenic Cooperative Oncology Group|Sanofi Bone Metastatic Prostate Cancer July 2015 Phase 2
NCT01830231 Associació per a la Recerca Oncologica, Spain Urothelium Transitional Cell Carcinoma October 2012 Phase 2|Phase 3
NCT01335204 Medical University of South Carolina|Peregrine Pharmaceuticals Prostate Cancer|Prostatic Neoplasms June 2011 Phase 1|Phase 2
NCT03043989 Sidney Kimmel Comprehensive Cancer Center Prostate Cancer March 21, 2017 Phase 1
NCT01650285 Brown University Prostate Cancer January 2013 Phase 2
NCT01254279 Sanofi Prostate Cancer Metastatic December 2010 Phase 3
NCT02478502 Jan Oldenburg|Sanofi|University Hospital, Akershus Testicular Cancer June 2015 Phase 2
NCT01740570 M.D. Anderson Cancer Center|Sanofi Brain Cancer April 2013 Phase 1|Phase 2
NCT01981668 Nova Scotia Cancer Centre|Sanofi Prostatic Neoplasms Phase 1
NCT01934894 SCRI Development Innovations, LLC|Novartis|GlaxoSmithKline|Sanofi Metastatic Breast Cancer With Intracranial Metastases November 2013 Phase 2
NCT02560337 Vejle Hospital Ovarian Cancer September 2015 Phase 2
NCT01845792 University of Colorado, Denver|Janssen Services, LLC Prostate Cancer July 2013 Phase 2
NCT02204332 Hospital Clinico Universitario de Santiago|Fundación Ramón Domínguez Colorectal Cancer March 2013 Phase 2
NCT01693549 Hellenic Cooperative Oncology Group|Sanofi Breast Cancer September 2012 Phase 2
NCT01941550 RWTH Aachen University High-Risk Cancer July 2013 Phase 2
NCT01913652 European Organisation for Research and Treatment of Cancer - EORTC|Sanofi Dedifferentiated Liposarcoma October 2014 Phase 2
NCT01750866 Case Comprehensive Cancer Center Castrate-resistant Metastatic Prostate Cancer February 2013 Phase 2
NCT01420250 Sidney Kimmel Cancer Center at Thomas Jefferson University|Sanofi|Thomas Jefferson University Prostate Cancer September 2011 Phase 1
NCT01757171 Weill Medical College of Cornell University|Sanofi Gastric Adenocarcinoma|Gastroesophageal Adenocarcinoma|Distal Esophageal Adenocarcinoma December 2012 Phase 2
NCT01620242 UNICANCER Recurrent Head and Neck Cancer|Metastatic Head and Neck Cancer April 2012 Phase 2
NCT01541007 Jeffrey Yachnin M.D., PhD.|Sanofi|Karolinska University Hospital Metastatic Castration Resistant Prostate Cancer April 2012 Phase 2
NCT01600339 Rambam Health Care Campus Urothelial Carcinoma May 2012 Phase 2
NCT01913067 Jules Bordet Institute|Sanofi Brain Metastasis|Breast Cancer|Non Small Cell Lung Cancer September 2013 Phase 2
NCT02166658 AIO-Studien-gGmbH|ClinAssess GmbH|Sanofi Breast Cancer|Lung Cancer|Recurrent Brain Metastases|Progressive Brain Metastases August 2015 Phase 2
NCT01751308 Sanofi Malignant Solid Tumor - Malignant Nervous System Neoplasm February 2013 Phase 1|Phase 2
NCT03114254 University Hospitals Bristol NHS Foundation Trust|Sanofi Penile Neoplasm December 5, 2014 Phase 2
NCT01001221 Sanofi Neoplasms, Malignant November 2009 Phase 1|Phase 2
NCT02202772 James M. McKiernan|Sanofi|Columbia University Urothelial Carcinoma of the Urinary Bladder December 2014 Phase 1
NCT01747239 Vejle Hospital|Sanofi Ovarian Cancer January 2013 Phase 2
NCT01527929 Sanofi Neoplasm Malignant April 2012 Phase 1
NCT01308580 Sanofi Prostate Cancer April 2011 Phase 3
NCT03048942 University Hospitals Bristol NHS Foundation Trust HER2 Negative Metastatic Breast Cancer November 2014 Phase 2
NCT01438307 University of Alabama at Birmingham|Sanofi Non-small Cell Lung Cancer (NSCLC)|Stage IV NSCLC|Metastatic NSCLC September 2011 Phase 2
NCT01956149 Prof. Dr. S.E. Al-Batran|Krankenhaus Nordwest Gastric Cancer September 2013 Phase 2
NCT01866449 University of Ulm Glioblastoma Multiforme (GBM) WHO Grade IV October 2013 Phase 2
NCT02035124 SCRI Development Innovations, LLC|Novartis Advanced Prostate Cancer April 2014 Phase 2
NCT01852578 Hellenic Oncology Research Group NSCLC September 2012 Phase 2
NCT01087021 Sanofi Neoplasms, Malignant March 2010 Phase 1
NCT02844582 University of California, Davis|Sanofi Hormone-Resistant Prostate Cancer|Stage IV Prostate Adenocarcinoma October 2016 Phase 2
NCT00925743 Sanofi Solid Cancer June 2009 Phase 1
NCT01500720 Sanofi Small Cell Lung Cancer March 2012 Phase 2
NCT02115165 Gustave Roussy, Cancer Campus, Grand Paris|Sanofi Non-seminomatous Germ-cell Tumors May 2014 Phase 2
NCT02621190 Erasmus Medical Center|Sanofi Prostatic Neoplasms February 2016 Phase 2
NCT01505868 M.D. Anderson Cancer Center|Sanofi Prostate Cancer July 2012 Phase 1|Phase 2
NCT01497964 Sanofi Gastric Cancer December 2011 Phase 1|Phase 2
NCT01616875 University Hospitals Bristol NHS Foundation Trust|Sanofi Infiltrating Bladder Urothelial Carcinoma May 2012 Phase 2
NCT01437488 Sidney Kimmel Cancer Center at Thomas Jefferson University|Sanofi|Thomas Jefferson University Urothelial Carcinoma February 16, 2012 Phase 2
NCT01952223 UNICANCER Adenocarcinoma of Prostate|Progression of Prostate Cancer September 2013 Phase 3
NCT01668459 Dr Anjali Zarkar|Sanofi|University Hospital Birmingham NHS Foundation Trust Transitional Cell Carcinoma January 2013 Phase 2|Phase 3
NCT01594918 Rahul Aggarwal|Sanofi|University of California, San Francisco Metastatic Castration-resistant Prostate Cancer June 2012 Phase 1
NCT01511536 Sanofi Prostate Cancer March 2012 Phase 1|Phase 2
NCT01755390 Sanofi Advanced Solid Tumor October 1999 Phase 1
NCT01578655 OncoGenex Technologies Prostate Cancer August 2012 Phase 3
NCT02254785 British Columbia Cancer Agency|Sanofi|Ozmosis Research Inc. Metastatic Castration-Resistant Prostatic Cancer October 2014 Phase 2
NCT01140607 Sanofi Neoplasm Malignant May 2010 Phase 1
NCT02961257 Association Pour La Recherche des Thérapeutiques Innovantes en Cancérologie Prostate Cancer Metastatic May 5, 2017 Phase 3
NCT02074137 Sanofi Prostate Cancer Metastatic July 2014 Phase 4
NCT01718353 Sanofi Prostate Cancer Metastatic March 2013 Phase 2
NCT02441894 Sanofi Prostate Cancer April 2015 Phase 4
NCT01379339 Krzysztof Misiukiewicz|Sanofi|Icahn School of Medicine at Mount Sinai Squamous Cell Carcinoma of the Head and Neck April 2011 Phase 1
NCT02522715 OHSU Knight Cancer Institute|National Cancer Institute (NCI) Hormone-Resistant Prostate Cancer|Metastatic Prostate Carcinoma|Recurrent Prostate Carcinoma|Stage IV Prostate Cancer June 2015 Phase 1|Phase 2
NCT03110588 University of Alabama at Birmingham|Astellas Pharma Inc|Sanofi Metastatic Prostate Cancer August 1, 2017 Phase 1
NCT02543255 University Health Network, Toronto Prostate Cancer September 2016 Phase 2
NCT02379390 Sanofi Prostate Cancer Metastatic June 2015 Phase 2
NCT02485691 Sanofi Prostate Cancer Metastatic November 2015 Phase 4
NCT02218606 Memorial Sloan Kettering Cancer Center|Sanofi|Thomas Jefferson University|Weill Medical College of Cornell University Prostate Cancer August 2014 Phase 2
NCT03050866 Erasmus Medical Center|Sanofi Circulating Tumor Cell|Metastatic Prostate Cancer February 21, 2017 Phase 2
NCT01308567 Sanofi Prostate Cancer May 2011 Phase 3
NCT00417079 Sanofi Neoplasms|Prostatic Neoplasms January 2007 Phase 3
NCT01649635 Sanofi Prostate Cancer July 2012 Phase 4
NCT01528163 Cliniques universitaires Saint-Luc- Université Catholique de Louvain Squamous Cell Carcinoma of the Head and Neck February 2012 Phase 2
NCT01576029 Sanofi Prostatic Neoplasms August 2012 Phase 2
NCT01324583 Sanofi Prostate Cancer January 2011 Phase 1
NCT01469338 University of Southern California|National Cancer Institute (NCI)|Sanofi Diarrhea|Hormone-resistant Prostate Cancer|Recurrent Prostate Cancer|Stage I Prostate Cancer|Stage IIA Prostate Cancer|Stage IIB Prostate Cancer|Stage III Prostate Cancer|Stage IV Prostate Cancer July 2012 Phase 2
NCT01978873 Örebro University, Sweden Prostate Cancer November 2012 Phase 3
NCT03101046 UNICANCER|National Cancer Institute, France|Institut du Cancer de Montpellier - Val d'Aurelle|Institut Bergonié Prostate Carcinoma|Castration-resistant Prostate Cancer|Circulating Tumor Cells|Chemotherapy October 1, 2017 Phase 2
NCT01083615 OncoGenex Technologies|Teva Pharmaceuticals USA Castrate-Resistant Prostate Cancer|Hormone Refractory Prostate Cancer March 2010 Phase 3
NCT01531205 H. Lee Moffitt Cancer Center and Research Institute|Sanofi Prostate Cancer May 2012 Phase 2
NCT02703623 M.D. Anderson Cancer Center|Bristol-Myers Squibb|Janssen, LP|Sanofi Prostate Cancer May 2016 Phase 2
NCT01447225 Merrimack Pharmaceuticals|Sanofi Solid Tumors October 2011 Phase 1
NCT02903160 Icahn School of Medicine at Mount Sinai|Sanofi|Bayer Prostate Cancer October 2016 Phase 2
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 1.1963 mL 5.9814 mL 11.9627 mL
5 mM 0.2393 mL 1.1963 mL 2.3925 mL
10 mM 0.1196 mL 0.5981 mL 1.1963 mL
Cell Assay
[1]

The cytotoxicity of CBX-loaded ANs and free Cabazitaxel (CBX) is evaluated with MTT assay. Cells are seeded onto a 96-well plate at a density of 3000 cells per well and cultured for 24 h. CBX-loaded ANs and free CBX are diluted to predetermined concentrations with PBS and added into each well. Blank AN, AN-ICG and free CBX solvent (a mixture of Tween-80 and anhydrous alcohol) are added as well to different final concentrations. The incubation continued for another 48 hours. 20 µL MTT solutions (5 mg/mL in PBS) are added into each well and cells are incubated for another 4 hours under 37°C. Subsequently the medium is removed and 150 µL dimethyl sulphoxide (DMSO) is added to dissolve the purple formazan salt crystals. Then the absorbance is measured by a microplate reader at 490 nm. The cells treated with medium are evaluated as controls.

Animal Administration
[1]

Cabazitaxel is dissolved in saline.

To evaluate the antitumor efficiency of the combined chemotherapy and PTT in vivo, mice bearing 4T1 tumor are randomLy divided into 6 treatment groups (n=5). Treatment begin when the tumors reached 50 mm3-100 mm3. 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 groups injected with AN-ICG and AN-ICG-CBX is irradiated by the 808 nm laser (0.8 W/cm2, 5 min). The length and width of every tumor are measured by a caliper every other day. The formula (volume (mm3) =1/2 × length × width2) is used to calculate the tumor volume. The body weights of these mice are recorded every two days using an electronic balance as well. At the end of the antitumor study, the 4T1 tumor bearing mice are sacrificed to collect the tumors and major organs.

References
M.Wt

835.93

Formula

C₄₅H₅₇NO₁₄

CAS No.

183133-96-2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Cabazitaxel
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