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Cabazitaxel(XRP-6258 RPR-116258A taxoid XRP6258)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Cabazitaxel(XRP-6258 RPR-116258A taxoid XRP6258)图片
CAS NO:183133-96-2
规格:≥98%
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
Cabazitaxel (formerly known as RPR-116258A, XRP-6258, TXD-258; Jevtana) is a semi-synthetic and marketed taxane analog (the natural taxoid 10-deacetylbaccatin III) with potential anticancer activity and improved pharmacological profiles (e.g. overcoming paclitaxel drug resistance). Cabazitaxel is an inhibitor of microtubule polymerization/microtubule stablizer which 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.
理化性质和储存条件
Molecular Weight (MW)835.93
FormulaC45H57NO14
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
Other info

Chemical Name: (2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-acetoxy-9-(((2R,3S)-3-((tert-butoxycarbonyl)amino)-2-hydroxy-3-phenylpropanoyl)oxy)-11-hydroxy-4,6-dimethoxy-4a,8,13,13-tetramethyl-5-oxo-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxet-12-yl benzoate.

InChi Key: BMQGVNUXMIRLCK-OAGWZNDDSA-N

InChi Code: InChI=1S/C45H57NO14/c1-24-28(57-39(51)33(48)32(26-17-13-11-14-18-26)46-40(52)60-41(3,4)5)22-45(53)37(58-38(50)27-19-15-12-16-20-27)35-43(8,36(49)34(55-10)31(24)42(45,6)7)29(54-9)21-30-44(35,23-56-30)59-25(2)47/h11-20,28-30,32-35,37,48,53H,21-23H2,1-10H3,(H,46,52)/t28-,29-,30+,32-,33+,34+,35-,37-,43+,44-,45+/m0/s1

SMILES Code: O=C(O[C@@H]([C@@]1([H])[C@@]2(C)[C@@H](OC)C[C@@]3([H])OC[C@]31OC(C)=O)[C@]4(O)C[C@H](OC([C@H](O)[C@@H](NC(OC(C)(C)C)=O)C5=CC=CC=C5)=O)C(C)=C(C4(C)C)[C@@H](OC)C2=O)C6=CC=CC=C6

SynonymsTXD 258; XRP6258; RPR116258A; TXD-258; RPR-116258A; TXD258; XRP-6258; TXD 258; XRP 6258; RPR-116258A; trade name: Jevtana.
实验参考方法
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).


Cell Assay: The cytotoxicity of CBX-loaded ANs and free Cabazitaxel (CBX) is evaluated with MTT assay. Cells are seeded onto a 96-well plate at a density of 3000 cells per well and cultured for 24 h. CBX-loaded ANs and free CBX are diluted to predetermined concentrations with PBS and added into each well. Blank AN, AN-ICG and free CBX solvent (a mixture of Tween-80 and anhydrous alcohol) are added as well to different final concentrations. The incubation continued for another 48 hours. 20 μL MTT solutions (5 mg/mL in PBS) are added into each well and cells are incubated for another 4 hours under 37°C. Subsequently the medium is removed and 150 μL dimethyl sulphoxide (DMSO) is added to dissolve the purple formazan salt crystals. Then the absorbance is measured by a microplate reader at 490 nm. The cells treated with medium are evaluated as controls.

In VivoIn 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 modelMurine tumor xenografts
Formulation & Dosage
ReferencesClin Interv Aging. 2010 Dec 3;5:395-402.