Name: Cabazitaxel
Brand: Selleck Chemicals
SKU: S3022
Availability: InStock
Rating: 5 (31 reviews)

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	Akt Wnt/beta-catenin HSP PKC ROCK Integrin Bcr-Abl Actin FAK Kinesin
Other Microtubule Associated Products	Nocodazole MMAF Patupilone (Epothilone B) Lexibulin (CYT997) CW069 Combretastatin A4 ABT-751 (E7010) Epothilone A Cucurbitacin B TAI-1

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
SGC7901	Growth inhibition assay		Growth inhibition of human SGC7901 cells by MTT assay, GI50=0.0003553μM	24405702
U937	Growth inhibition assay		Growth inhibition of human U937 cells by MTT assay, GI50=0.0005391μM	24405702
MCF7	Growth inhibition assay		Growth inhibition of human MCF7 cells by MTT assay, GI50=0.001187μM	24405702
PANC1	Growth inhibition assay		Growth inhibition of human PANC1 cells by MTT assay, GI50=0.001283μM	24405702
HT1080	Growth inhibition assay		Growth inhibition of human HT1080 cells by MTT assay, GI50=0.001406μM	24405702
DU145	Growth inhibition assay		Growth inhibition of human DU145 cells by MTT assay, GI50=0.001429μM	24405702
A549	Growth inhibition assay		Growth inhibition of human A549 cells by MTT assay, GI50=0.001483μM	24405702
A431	Growth inhibition assay		Growth inhibition of human A431 cells by MTT assay, GI50=0.001483μM	24405702
HeLa	Growth inhibition assay		Growth inhibition of human HeLa cells by MTT assay, GI50=0.001799μM	24405702
K562	Growth inhibition assay		Growth inhibition of human K562 cells by MTT assay, GI50=0.004186μM	24405702
HL60	Growth inhibition assay		Growth inhibition of human HL60 cells by MTT assay, GI50=0.004736μM	24405702
BGC823	Growth inhibition assay		Growth inhibition of human BGC823 cells by MTT assay, GI50=0.4672μM	24405702
A549	Cytotoxicity assay		Cytotoxicity against human A549 cells, IC50=0.00148μM	28850227
MES-SA/Dx5	Growth inhibition assay	72 hrs	Growth inhibition of human MES-SA/Dx5 cells after 72 hrs by SRB assay, IC50=0.015μM	29251920
TC32	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
Saos-2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
LAN-5	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
OHS-50	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
Rh41	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
SK-N-MC	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
TC32	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
MG 63 (6-TG R)	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	29435139
U-2 OS	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
Rh41	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
Saos-2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	29435139
OHS-50	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells	29435139
NCI-H524	Cytotoxicity assay	2 hrs	Cytotoxicity in human NCI-H524 cells pre-incubated for 2 hrs followed by compound wash out and subsequently incubated for 70 hrs by Cell Titer Glo assay, IC50=0.00026μM	30735385
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 167 mg/mL (199.77 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (5.98mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.250mg/ml (1.50mM)	Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	835.93	Formula	C₄₅H₅₇NO₁₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	183133-96-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	XRP6258, RPR-116258A, TXD 258, Taxoid XRP6258			Smiles	CC1=C2C(C(=O)C3(C(CC4C(C3C(C(C2(C)C)(CC1OC(=O)C(C(C5=CC=CC=C5)NC(=O)OC(C)(C)C)O)O)OC(=O)C6=CC=CC=C6)(CO4)OC(=O)C)OC)C)OC

Mechanism of Action

Features	A semi-synthetic derivative of a natural taxoid.
Targets/IC₅₀/Ki	Microtubule (Cell-free assay)
In vitro	Cabazitaxel increases CYP3A enzyme activities in rat hepatocytes. The mean ex-vivo human plasma protein binding of this compound is 91.6%. It is rapidly and extensively metabolised in numerous metabolites. This compound demonstrates activity in several murine and human resistant cell lines. With a 4-day exposure to this chemical, cytotoxicity is noted with relatively low cabazitaxel concentrations. It 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), this compound elicites complete tumor regressions. Using SF-295 and U251 human glioblastoma cell lines, both orthotopic and subcutaneous murine xenografts are generated. This chemical treatment leads to complete regression in the majority of subcutaneously implanted tumors. Furthermore, in orthotopic models, it leads to complete tumor regression in 4 out of 10 U251 tumors.
References	[1] http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Public_assessment_report/human/002018/WC500104766.pdf [2] https://pubmed.ncbi.nlm.nih.gov/21152241/ [3] https://pubmed.ncbi.nlm.nih.gov/36123339/ [4] https://pubmed.ncbi.nlm.nih.gov/27608834/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04622761	Not yet recruiting	Prostate Cancer	The Clatterbridge Cancer Centre NHS Foundation Trust\|University of Liverpool	January 15 2021	Phase 2
NCT04495179	Completed	Progressive Metastatic Castrate-Resistant Prostate Cancer	AstraZeneca\|Parexel	August 4 2020	Phase 2
NCT03257891	Unknown status	Adrenocortical Carcinoma	Azienda Socio Sanitaria Territoriale degli Spedali Civili di Brescia\|San Luigi Gonzaga Hospital	January 25 2018	Phase 2
NCT03043989	Terminated	Prostate Cancer	Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins\|Maryland Technology Development Corporation	March 21 2017	Phase 1

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Frequently Asked Questions

Question 1:
What is the elimination half-life of this compound?

Answer:
According to the paper report, its elimination half-life is 95h.

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Cabazitaxel Microtubule Associated inhibitor

Chemical Structure

Molecular Weight: 835.93