Cabazitaxel (XRP6258)

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

For research use only.

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.

Cabazitaxel (XRP6258) Chemical Structure

CAS No. 183133-96-2

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

Purity & Quality Control

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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 MV7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NF\VXlZIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBUT0N5OUCxJINmdGy|IHL5JG1VXCCjc4PhfUwhT0l3ME2wMlAxODN3NUROwG0> MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRyNUewNkc,OjR2MEW3NFI9N2F-
U937 M4jt[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXm3TphwT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hXTl|NzDj[YxteyCkeTDNWHQh[XO|YYmsJGdKPTB;MD6wNFA2OzlzzszN M4XoOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEC1O|AzLz5{NESwOVcxOjxxYU6=
MCF7 M3r6OWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{LzdWdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJG1ETjdiY3XscJMh[nliTWTUJIF{e2G7LDDHTVUxRTBwMECxNVg4|ryP MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRyNUewNkc,OjR2MEW3NFI9N2F-
PANC1 M13wdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlHFS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gVGFPSzFiY3XscJMh[nliTWTUJIF{e2G7LDDHTVUxRTBwMECxNlg{|ryP MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRyNUewNkc,OjR2MEW3NFI9N2F-
HT1080 M2POOWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFPF[XBIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJXDFyOECgZ4VtdHNiYomgUXRVKGG|c3H5MEBIUTVyPUCuNFAyPDB4zszN NF\QNXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESwOVcxOid-MkS0NFU4ODJ:L3G+
DU145 MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXLRS5VTT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hTFVzNEWgZ4VtdHNiYomgUXRVKGG|c3H5MEBIUTVyPUCuNFAyPDJ7zszN NETCfoY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESwOVcxOid-MkS0NFU4ODJ:L3G+
A549 MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{jndmdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGE2PDliY3XscJMh[nliTWTUJIF{e2G7LDDHTVUxRTBwMECxOFg{|ryP M2POZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEC1O|AzLz5{NESwOVcxOjxxYU6=
A431 MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{PxOWdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGE1OzFiY3XscJMh[nliTWTUJIF{e2G7LDDHTVUxRTBwMECxOFg{|ryP NYjlO4NzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0NFU4ODJpPkK0OFA2PzB{PD;hQi=>
HeLa Mon5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGq4RYxIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJ\UyjIHPlcIx{KGK7IF3UWEBie3OjeTygS2k2OD1yLkCwNVc6Qc7:TR?= NXrVd3F2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0NFU4ODJpPkK0OFA2PzB{PD;hQi=>
K562 MUDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXzHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDLOVYzKGOnbHzzJIJ6KE2WVDDhd5NigSxiR1m1NF0xNjByNEG4Ou69VQ>? MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRyNUewNkc,OjR2MEW3NFI9N2F-
HL60 MnnoS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MonwS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gTGw3OCClZXzsd{BjgSCPVGSgZZN{[XluIFfJOVA:OC5yMES3N|bPxE1? NVPXXVFbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0NFU4ODJpPkK0OFA2PzB{PD;hQi=>
BGC823 NWDsOINDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWLucIVRT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hSkeFOEKzJINmdGy|IHL5JG1VXCCjc4PhfUwhT0l3ME2wMlQ3PzMQvF2= NEmw[Gc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESwOVcxOid-MkS0NFU4ODJ:L3G+
A549 NGLSepNEgXSxdH;4bYNqfHliYYPzZZk> M1HtcWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE2PDliY3XscJMtKEmFNUC9NE4xODF2ON88US=> NVz2VWhjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki4OVAzOjdpPkK4PFUxOjJ5PD;hQi=>
MES-SA/Dx5 NEXR[WZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2XsNVczKGi{cx?= NHq3TZlIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBOTVNvU1GvSJg2KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDTVmIh[XO|YYmsJGlEPTB;MD6wNVXPxE1? NELIVZk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUK1NVkzOCd-MkmyOVE6OjB:L3G+
TC32 NVnGOIY3eUiWUzDhd5NigQ>? NInxR4ZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiVFOzNkBk\Wyucx?= MlfrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
A673 M{HkTpFJXFNiYYPzZZk> MVrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? MoHvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC M{fYS5FJXFNiYYPzZZk> Mn;jdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= NEnuRng9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Saos-2 M1\0ZZFJXFNiYYPzZZk> MVvxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy| M{LITFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
LAN-5 M4DtOJFJXFNiYYPzZZk> NYj4V3FOeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFzBUk02KGOnbHzz NUS2bIx1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
OHS-50 Mo[4dWhVWyCjc4PhfS=> NWTlVINteUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF;IV{02OCClZXzsdy=> MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh41 MXHxTHRUKGG|c3H5 MkHBdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqNEGgZ4VtdHN? NIPDZnI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
A673 NIHTdoxyUFSVIHHzd4F6 M2PXO5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJGE3PzNiY3XscJMq MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-MC M1fTeZFJXFNiYYPzZZk> MVrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDTT{1PNU2FIHPlcIx{ NVT1U4IyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
TC32 M2S2dZFJXFNiYYPzZZk> M3v0bJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHREOzJiY3XscJM> NF3mV5Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
MG 63 (6-TG R) NXPBcnNueUiWUzDhd5NigQ>? MYTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDNS{A3OyBqNj3US{BTMSClZXzsdy=> NH\ReYI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
U-2 OS NF7ocVNyUFSVIHHzd4F6 NFK3XmhyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBWNTJiT2OgZ4VtdHN? MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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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 (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 835.93
Formula

C45H57NO14

CAS No. 183133-96-2
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Molarity Calculator

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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 Active not recruiting Drug: AZD4635|Drug: Durvalumab|Drug: Cabazitaxel Progressive Metastatic Castrate-Resistant Prostate Cancer AstraZeneca|Parexel August 4 2020 Phase 2
NCT03257891 Unknown status 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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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.

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