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Cabazitaxel (XRP6258)
Catalog No.S3022 Synonyms: RPR-116258A, TXD 258, Taxoid XRP6258
For research use only.
Cabazitaxel (RPR-116258A, XRP6258, TXD 258, Taxoid XRP6258) 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.
CAS No. 183133-96-2
Selleck's Cabazitaxel (XRP6258) has been cited by 22 publications
Purity & Quality Control
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Biological Activity
| Description | Cabazitaxel (RPR-116258A, XRP6258, TXD 258, Taxoid XRP6258) 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. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Features | A semi-synthetic derivative of a natural taxoid. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Targets |
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| 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] |
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| Cell Data |
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| 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] |
Protocol (from reference)
Solubility (25°C)
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In vitro |
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Chemical Information
| Molecular Weight | 835.93 | ||
|---|---|---|---|
| Formula | C45H57NO14 |
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| CAS No. | 183133-96-2 | ||
| Storage | 3 years | -20°C | powder |
| 2 years | -80°C | in solvent | |
| 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 | ||
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Clinical Trial Information
| NCT Number | Recruitment | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT04622761 | Not yet recruiting | Drug: Cabazitaxel | Prostate Cancer | The Clatterbridge Cancer Centre NHS Foundation Trust|University of Liverpool | January 15 2021 | Phase 2 |
| NCT04495179 | Active not recruiting | Drug: AZD4635|Drug: Durvalumab|Drug: Cabazitaxel | Progressive Metastatic Castrate-Resistant Prostate Cancer | AstraZeneca|Parexel | August 4 2020 | Phase 2 |
| NCT03257891 | Unknown status | Drug: Cabazitaxel | Adrenocortical Carcinoma | Azienda Socio Sanitaria Territoriale degli Spedali Civili di Brescia|San Luigi Gonzaga Hospital | January 25 2018 | Phase 2 |
| NCT03043989 | Terminated | Drug: Docetaxel|Drug: Cabazitaxel|Drug: Clarithromycin | Prostate Cancer | Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Maryland Technology Development Corporation | March 21 2017 | Phase 1 |
(data from https://clinicaltrials.gov, updated on 2022-08-01)
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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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