MK-8745 885325-71-3

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Molecular Weight: 431.91 MK-8745 is a potent and selective Aurora A inhibitor with IC50 of 0.6 nM, more than 450-fold selectivity for Aurora A over Aurora B.


Biological Activity


MK-8745
leads to Cell Cycle arrest at the G2/M phase with accumulation of
tetraploid nuclei followed by cell death in non-Hodgkin lymphoma (NHL)
cell lines. Treatment with MK-8745 induces p21(waf1/cip1) and CycB1,
indicating cell cycle arrest and an increase in the G2/M phase cell
population. Following MK-8745 treatment, Aurora-A substrates (TACC3, Eg5
and TPX2) are rapidly degraded following the reduction of
phospho-Aurora-A. MK8745 induces apoptotic cell death in a
p53-dependent manner when tested in vitro in cell lines of multiple
lineages. Exposure of p53 wild-type cells to MK8745 results in the
induction of p53 phosphorylation (ser15) and an increase in p53 protein
expression. p53-dependent Apoptosis by MK8745 is further confirmed in
HCT 116 p53(-/-) cells transfected with wild-type p53.


Protocol(Only for Reference)


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

Molecular Weight (MW)	431.91
Formula	C20 H19 Cl F N5 O S
CAS No.	885325-71-3

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

Solubility (25°C) *	In vitro	DMSO	86 mg/mL (199.11 mM)
		Water	<1 mg/mL (
		Ethanol	1 mg/mL (2.31 mM)
* <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	Methanone, (3-chloro-2-fluorophenyl)[4-[[6-(2-thiazolylamino)-2-pyridinyl]methyl]-1-piperazinyl]-

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Product Categories : Epigenetics > Aurora Kinase Inhibitor