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    Cabazitaxel (XRP-6258; RPR-116258A; taxoid XRP6258)
    Cabazitaxel (XRP-6258; RPR-116258A; taxoid XRP6258)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1609
    CAS #: 183133-96-2Purity ≥98%

    Description: 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. 

    References: Clin Interv Aging. 2010 Dec 3;5:395-402.  

    Related CAS #: 183133-96-2 (Cabazitaxel)    1383572-18-6 (d3)    1383561-29-2 (d6)   1383572-17-5 

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    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[[email protected]@H]([[email protected]@]1([H])[[email protected]@]2(C)[[email protected]@H](OC)C[[email protected]@]3([H])OC[[email protected]]31OC(C)=O)[[email protected]]4(O)C[[email protected]](OC([[email protected]](O)[[email protected]@H](NC(OC(C)(C)C)=O)C5=CC=CC=C5)=O)C(C)=C(C4(C)C)[[email protected]@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.


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    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.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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