Cabazitaxel

Catalog No.S3022 Batch:S302202

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Technical Data

Formula

C45H57NO14
Molecular Weight 835.93 CAS No. 183133-96-2
Solubility (25°C)* In vitro DMSO 167 mg/mL (199.77 mM)
Water Insoluble
Ethanol Insoluble
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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.
Targets
Microtubule [1]
(Cell-free assay)
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 (from reference)

Cell Assay:

[3]
  • Cell lines

    TFK1 cells

  • Concentrations

    0.25 μM

  • Incubation Time

    24 h

  • Method

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

Customer Product Validation

, , Mol Cancer Ther, 2017, 16(10):2257-2266

, , Urol Oncol, 2015, 33(9):385.e15-20.

Data from [Data independently produced by , , Cell, 2018, 174(5):1200-1215]

Data from [Data independently produced by , , Clin Cancer Res, 2018, doi:10.1158/1078-0432.CCR-18-0704]

Selleck's Cabazitaxel has been cited by 29 publications

Fabrication of hyaluronic acid-altered gold complex delivery for head and neck squamous cell carcinoma therapy with high antitumor efficacy and low in vivo toxicity [ J Photochem Photobiol B, 2024, 253:112877] PubMed: 38484648
Association between the apoptotic effect of Cabazitaxel and its pro-oxidant efficacy on the redox adaptation mechanisms in prostate cancer cells with different resistance phenotypes [ Cancer Biol Ther, 2024, 25(1):2329368] PubMed: 38485703
Targeting prostate tumor low-molecular weight tyrosine phosphatase for oxidation-sensitizing therapy [ Sci Adv, 2024, 10(5):eadg7887] PubMed: 38295166
Ritonavir reverses resistance to docetaxel and cabazitaxel in prostate cancer cells with acquired resistance to docetaxel [ Cancer Drug Resist, 2024, 7:3] PubMed: 38318527
Relevance of the organic anion transporting polypeptide 1B3 (OATP1B3) in the personalized pharmacological treatment of hepatocellular carcinoma [ Biochem Pharmacol, 2023, 214:115681] PubMed: 37429423
Berbamine targets cancer stem cells and reverses cabazitaxel resistance via inhibiting IGF2BP1 and p-STAT3 in prostate cancer [ Prostate, 2023, 10.1002/pros.24632] PubMed: 37828768
The therapeutic effect of KSP inhibitors in preclinical models of cholangiocarcinoma [ Cell Death Dis, 2022, 13-9:799] PubMed: 36123339
Activation of the ABCB1-amplicon promotes cellular viability and resistance to docetaxel and cabazitaxel in castration-resistant prostate cancer [ Mol Cancer Ther, 2021, molcanther.0983.2020] PubMed: 34326198
Proteomic analysis of extracellular vesicles identified PI3K pathway as a potential therapeutic target for cabazitaxel-resistant prostate cancer [ Prostate, 2021, 10.1002/pros.24138] PubMed: 33905554
DNA-PKc inhibition overcomes taxane resistance by promoting taxane-induced DNA damage in prostate cancer cells [ Prostate, 2021, 10.1002/pros.24200] PubMed: 34297853

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.