Cabazitaxel (XRP6258)

For research use only.

Catalog No.S3022 Synonyms: RPR-116258A, TXD 258, Taxoid XRP6258

22 publications

Cabazitaxel (XRP6258) Chemical Structure

CAS No. 183133-96-2

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.

Selleck's Cabazitaxel (XRP6258) has been cited by 22 publications

Purity & Quality Control

Choose Selective Microtubule Associated Inhibitors

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.
Features A semi-synthetic derivative of a natural taxoid.
Targets
Microtubule [1]
(Cell-free assay)
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SGC7901 M33ofWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlG0S5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gV2dEPzlyMTDj[YxteyCkeTDNWHQh[XO|YYmsJGdKPTB;MD6wNFA{PTV|zszN NYTzRpBLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0NFU4ODJpPkK0OFA2PzB{PD;hQi=>
U937 MWLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Ml\JS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gWVk{PyClZXzsd{BjgSCPVGSgZZN{[XluIFfJOVA:OC5yMEC1N|ky|ryP M3zwVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEC1O|AzLz5{NESwOVcxOjxxYU6=
MCF7 MnjCS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Ml;pS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUWNHPyClZXzsd{BjgSCPVGSgZZN{[XluIFfJOVA:OC5yMEGxPFfPxE1? MmnTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2MEW3NFIoRjJ2NEC1O|AzRC:jPh?=
PANC1 M2rz[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUHHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDQRW5EOSClZXzsd{BjgSCPVGSgZZN{[XluIFfJOVA:OC5yMEGyPFPPxE1? MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRyNUewNkc,OjR2MEW3NFI9N2F-
HT1080 M4niRWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NF3nPHFIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJXDFyOECgZ4VtdHNiYomgUXRVKGG|c3H5MEBIUTVyPUCuNFAyPDB4zszN NFeydnk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESwOVcxOid-MkS0NFU4ODJ:L3G+
DU145 NXvJSFBKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NV\JXZNbT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hTFVzNEWgZ4VtdHNiYomgUXRVKGG|c3H5MEBIUTVyPUCuNFAyPDJ7zszN MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRyNUewNkc,OjR2MEW3NFI9N2F-
A549 MU\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVHHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDBOVQ6KGOnbHzzJIJ6KE2WVDDhd5NigSxiR1m1NF0xNjByMUS4N:69VQ>? NIP1SXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESwOVcxOid-MkS0NFU4ODJ:L3G+
A431 M1\wSGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWrDUXcyT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hSTR|MTDj[YxteyCkeTDNWHQh[XO|YYmsJGdKPTB;MD6wNFE1QDQQvF2= NXO5NpdORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0NFU4ODJpPkK0OFA2PzB{PD;hQi=>
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K562 MnHaS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NV3WWFN1T3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUzV4MjDj[YxteyCkeTDNWHQh[XO|YYmsJGdKPTB;MD6wNFQyQDcQvF2= MoHrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2MEW3NFIoRjJ2NEC1O|AzRC:jPh?=
HL60 NIG0dIZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mlq0S5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gTGw3OCClZXzsd{BjgSCPVGSgZZN{[XluIFfJOVA:OC5yMES3N|bPxE1? MnjUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2MEW3NFIoRjJ2NEC1O|AzRC:jPh?=
BGC823 NHTVb5VIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUHHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDCS2M5OjNiY3XscJMh[nliTWTUJIF{e2G7LDDHTVUxRTBwNE[3Nu69VQ>? MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRyNUewNkc,OjR2MEW3NFI9N2F-
A549 M2\obWN6fG:2b4jpZ4l1gSCjc4PhfS=> NFPNdGZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{NCCLQ{WwQVAvODBzNElOwG0> NWjueoNlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki4OVAzOjdpPkK4PFUxOjJ5PD;hQi=>
MES-SA/Dx5 Mmq0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mk\OO|IhcHK| NYXmRmtNT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVUWVLWPBM2R5PSClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUCuNFE2|ryP M2LCU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MkWxPVIxLz5{OUK1NVkzODxxYU6=
TC32 NX[xNmpUeUiWUzDhd5NigQ>? M2nDR5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCWQ{OyJINmdGy| NEjhTo09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
A673 NFW2fWlyUFSVIHHzd4F6 Mm\4dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEF4N{OgZ4VtdHN? NEjseGU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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LAN-5 MYLxTHRUKGG|c3H5 NEOyUWZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTFHOMVUh[2WubIO= M2f1c|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
OHS-50 NH6zbHVyUFSVIHHzd4F6 M4rxc5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCRSGOtOVAh[2WubIO= NYm3SmQ6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh41 M3L5RZFJXFNiYYPzZZk> MYXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmh2MTDj[Yxtew>? Ml7FQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
A673 M2PZV5FJXFNiYYPzZZk> M2LIVpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJGE3PzNiY3XscJMq NWPhcoFwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC NX31RYRqeUiWUzDhd5NigQ>? MX3xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDTT{1PNU2FIHPlcIx{ MofvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
TC32 NXrBRnZteUiWUzDhd5NigQ>? M37CNZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHREOzJiY3XscJM> MlrqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
MG 63 (6-TG R) MYjxTHRUKGG|c3H5 MkmwdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgUWchPjNiKE[tWGchWiliY3XscJM> MoPEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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... Click to View More Cell Line Experimental Data

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

Solubility (25°C)

In vitro DMSO 100 mg/mL (119.62 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 835.93
Formula

C45H57NO14

CAS No. 183133-96-2
Storage powder
in solvent
Synonyms RPR-116258A, TXD 258, Taxoid XRP6258
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 Recruiting Drug: AZD4635|Drug: Durvalumab|Drug: Cabazitaxel Progressive Metastatic Castrate-Resistant Prostate Cancer AstraZeneca|Parexel August 4 2020 Phase 2
NCT03257891 Recruiting 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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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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.

Microtubule Associated Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID