Home Cytoskeletal Signaling Microtubule Associated inhibitor - Autophagy activator Cabazitaxel For research use only.

Cabazitaxel

Synonyms: XRP6258, RPR-116258A, TXD 258, Taxoid XRP6258

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. Cabazitaxel induces autophagy via the PI3K/Akt/mTOR pathway.

Cabazitaxel Chemical Structure

Cabazitaxel Chemical Structure

CAS No. 183133-96-2

Purity & Quality Control

Cabazitaxel Related Products

Signaling Pathway

Microtubule Associated Signaling Pathways

Microtubule Associated Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation 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

Biological Activity

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. Cabazitaxel induces autophagy via the PI3K/Akt/mTOR pathway.
Features A semi-synthetic derivative of a natural taxoid.
Targets
Microtubule [1]
(Cell-free assay)
In vitro
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]
Cell Research Cell lines TFK1 cells
Concentrations 0.25 μM
Incubation Time 24 h
Method

Cells were treated with various concentrations of drug for 24 h.
In Vivo
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]
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

Chemical Information & Solubility

Molecular Weight 835.93 Formula

C45H57NO14
CAS No. 183133-96-2 SDF Download Cabazitaxel SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 167 mg/mL ( (199.77 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

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.

Handling Instructions

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Frequently Asked Questions

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

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

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