Cabazitaxel 183133-96-2

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Molecular Weight:

835.93 Cabazitaxel (XRP6258) is a semi-synthetic derivative of a natural taxoid.


Biological 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).


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.


Protocol(Only for Reference)


Animal Study: [2]

Animal Models	Murine tumor xenografts (colon C38 and pancreas P03)
Formulation
Dosages
Administration

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Download Cabazitaxel SDF

Molecular Weight (MW)	835.93
Formula	C45H57NO14
CAS No.	183133-96-2

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms

Solubility (25°C) *	In vitro	DMSO	100 mg/mL (119.62 mM)
		Water	<1 mg/mL (
		Ethanol	<1 mg/mL (
* <1 mg/ml means slightly soluble or 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 Name	Benzenepropanoic acid, β-[[(1,1-dimethylethoxy)carbonyl]amino]-α-hydroxy-, (2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-(acetyloxy)-12-(benzoyloxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-11-hydroxy-4,6-dimethoxy-4a,8,13,13-tetramethyl-5-oxo-7,11-methano-1H-cyclodeca[3,4]benz[1,2-b]oxet-9-yl ester, (αR,βS)-

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