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Cabazitaxel

(CAS No:183133-96-2)

Cabazitaxel 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.

CAS No:183133-96-2

Molecular Weight(MW):835.93

Purity:98%+

Specification:500mg;1g;5g;10g;50g;100g

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QC Documents

COA	MSDS	HPLC	NMR

ChemicalInfomation

CAS No:	183133-96-2
Molecular formula(MF)	C₄₅H₅₇NO₁₄
Molecular Weight(MW):	835.93
Alias

Solubility

In vitro	DMSO	100 mg/mL (119.62 mM)
	Water	<1 mg/mL
	Ethanol	<1 mg/mL
In vivo

Biological Activity

Description

Cabazitaxel 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.

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	Activity Description	PMID
human MCF7 cells	Growth inhibition assay	Growth inhibition of human MCF7 cells by MTT assay, GI50=1.19 nM	24405702
human DU145 cells	Growth inhibition assay	Growth inhibition of human DU145 cells by MTT assay, IC50=1.43 nM	24405702
human A549 cells	Growth inhibition assay	Growth inhibition of human A549 cells by MTT assay, IC50=1.48 nM	24405702
human A431 cells	Growth inhibition assay	Growth inhibition of human A431 cells by MTT assay, IC50=1.48 nM	24405702
human HeLa cells	Growth inhibition assay	Growth inhibition of human HeLa cells by MTT assayï¼ IC50=1.8 nM	24405702
human K562 cells	Growth inhibition assay	Growth inhibition of human K562 cells by MTT assay	24405702
human HL60 cells	Growth inhibition assay	Growth inhibition of human HL60 cells by MTT assay	24405702

... 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]