Cabazitaxel

Catalog No.S3022

Cabazitaxel (XRP6258) is a semi-synthetic derivative of a natural taxoid.

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Cabazitaxel  Chemical Structure

Cabazitaxel Chemical Structure
Molecular Weight: 835.93

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Cabazitaxel is available in the following compound libraries:

Product Information

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Product Description

Biological Activity

Description Cabazitaxel (XRP6258) is a semi-synthetic derivative of a natural taxoid.
Targets Microtubule [1]
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]
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]
Features A semi-synthetic derivative of a natural taxoid.

Protocol(Only for Reference)

Animal Study: [2]

Animal Models Murine tumor xenografts (colon C38 and pancreas P03)
Formulation
Dosages
Administration

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] EMEA/H/C/002018, 2011.

[2] Pal SK, et al. Clin Interv Aging, 2010, 5, 395-402.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2014-01-26)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02166658 Not yet recruiting Breast Cancer|Lung Cancer|Recurrent Brain Metastases|Progressive Brain Metastases AIO-Studien-gGmbH|ClinAssess GmbH|Sanofi January 2015 Phase 2
NCT02166658 Not yet recruiting Breast Cancer|Lung Cancer|Recurrent Brain Metastases|Progressive Brain Metastases AIO-Studien-gGmbH|ClinAssess GmbH|Sanofi January 2015 Phase 2
NCT01913652 Recruiting Dedifferentiated Liposarcoma European Organisation for Research and Treatment of Cance  ...more European Organisation for Research and Treatment of Cancer - EORTC|Sanofi October 2014 Phase 2
NCT02254785 Not yet recruiting Metastatic Castration-Resistant Prostatic Cancer British Columbia Cancer Agency|Sanofi|Ozmosis Research Inc. October 2014 Phase 2
NCT01913652 Recruiting Dedifferentiated Liposarcoma European Organisation for Research and Treatment of Cance  ...more European Organisation for Research and Treatment of Cancer - EORTC|Sanofi October 2014 Phase 2

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Chemical Information

Download Cabazitaxel SDF
Molecular Weight (MW) 835.93
Formula

C45H57NO14

CAS No. 183133-96-2
Storage 3 years -20℃Powder
6 months-80℃in solvent (DMSO, water, etc.)
Synonyms
Solubility (25°C) * In vitro DMSO 100 mg/mL (119.62 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 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.
Chemical Name Benzenepropanoic acid, β-[[(1,1-dimethylethoxy)carbonyl]amino]-α-hydroxy-, (2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-(acetyloxy)-12-(benzoyloxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-11-hydroxy-4,6-dimethoxy-4a,8,13,13-tetramethyl-5-oxo-7,11-methano-1H-cyclodeca[3,4]benz[1,2-b]oxet-9-yl ester, (αR,βS)-

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