product name Cabazitaxel
Description: Cabazitaxel (also known as RPR-116258A, XRP6258, TXD 258) is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential anticancer activity. Cabazitaxel binds to and stabilizes tubulin, resulting in the inhibition of microtubule depolymerization and cell division, cell cycle arrest in the G2/M phase, and the inhibition of tumor cell proliferation. Unlike other taxane compounds, this agent is a poor substrate for the membrane-associated, multidrug resistance (MDR), P-glycoprotein (P-gp) efflux pump and may be useful for treating multidrug-resistant tumors.
References: Clin Interv Aging. 2010 Dec 3;5:395-402.
835.93
Formula
C45H57NO14
CAS No.
183133-96-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (119.6 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
RPR-116258A, XRP6258, TXD 258
other peoduct :
| In Vitro |
In vitro activity: 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). Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | |
| Formulation & Dosage | |
| References | Clin Interv Aging. 2010 Dec 3;5:395-402. |
