Cabazitaxel (XRP6258) - Moligand™, 10mM in DMSO , Inhibitor of tubulin beta class I, CAS No.183133-96-2, Inhibitor of tubulin beta class I

CAS: 183133-96-2 Cat. No.: C408885 Molecular Weight: 835.93 EC Number: 680-632-7

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

RPR-116258A, TXD 258, Taxoid XRP6258 | 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

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Cabazitaxel (XRP6258) 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
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. 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).

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.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyms

RPR-116258A, TXD 258, Taxoid XRP6258 | 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

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

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, pr

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Inhibitor of tubulin beta class I

Product Properties

• ALogP: 2.7

Names and Identifiers

• Isomeric SMILES: CC1=C2[C@H](C(=O)[C@@]3([C@H](C[C@@H]4[C@]([C@H]3[C@@H]([C@@](C2(C)C)(C[C@@H]1OC(=O)[C@@H]([C@H](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
• Molecular Weight: 835.93
• Reaxy-Rn: 24865959
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=24865959&ln=

Associated Targets(Human)

TUBB Tclin Tubulin beta chain (0 Activities)

Discover Target: TUBB

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Melt Point(°C): 180°C

References

1. P. Baby Shakila, Abdurahman Hajinur Hirad, Abdullah A. Alarfaj, Samer Hasan Hussein-Al-Ali, Beza Mulugeta.  (2023)  Precise Construction of Dual-Promising Anticancer Drugs Associated with Gold Nanomaterials on Glioma Cancer Cells.  BIOINORGANIC CHEMISTRY AND APPLICATIONS,      [PMID:37920234] [10.1155/2023/8892099]

2. Chen Guo, Haoyang Yuan, Ying Yu, Zhencheng Gao, Yu Zhang, Tian Yin, Haibing He, Jingxin Gou, Xing Tang.  (2023)  FRET-based analysis on the structural stability of polymeric micelles: Another key attribute beyond PEG coverage and particle size affecting the blood clearance.  JOURNAL OF CONTROLLED RELEASE,      [PMID:37454913] [10.1016/j.jconrel.2023.07.026]

3. Jianming Gong, Renqian Feng, Xiaoqing Fu, Qi Lin, Bicheng Wu.  (2024)  Fabrication of co-delivery liposomal formulation incorporating carmustine and cabazitaxel displays improved cytotoxic potential and induced apoptosis in ovarian cancer cells.  JOURNAL OF BIOMATERIALS SCIENCE-POLYMER EDITION,      [PMID:39207251] [10.1080/09205063.2024.2387949]