MK8745 Property

Melting point:

177-179°C

Boiling point:

605.5±65.0 °C(Predicted)

Density 

1.430±0.06 g/cm3(Predicted)

storage temp. 

Refrigerator

solubility 

DMSO (Slightly), Methanol (Slightly, Heated)

form 

Solid

pka

5.20±0.10(Predicted)

color 

Off-White

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

MK8745 Chemical Properties,Usage,Production

Uses

MK-8745 is a potent and selective Aurora A kinase inhibitor that induces apoptotic cell death in a p53-dependent manner when tested in vitro in cell lines of multiple lineages.

Biological Activity

mk-8745 is a novel and selective inhibitor of aurora a with ic50 value of 0.6 nm [1].aurora a kinase is a member of mitotic serine/threonine kinases and plays an important role in cellular division by controlling chromatid segregation. it has been reported that abnormal expression of aurora a is correlated with the high occurrence of cancer and its expression determines cell sensitivity to mk-8745 treatment [1].mk-8745 is a potent aurora a inhibitor. when tested with p53-/+ cell lines, mk-8745 treatment induced apoptotic cell death in a p53-dependent manner through inhibiting aurora a activity [1]. in non-hodgkin lymphoma (nhl) cell lines, mk-8745 treatment arrested cell cycle in g2/m phase and induced cell death via inhibiting aurora a kinase [2]. in hct 116 puma (-), hct116 p21 (-), hct116 bax(-) and hct116 chk2(-) cell lines, mk-8745 treatment induced cell apoptosis with the percent of 25%, 22%, 25%, and 22%, respectively [3].in female athymic nude mice model subcutaneous xenografted with hct116 puma (-), hct116 p21 (-), hct116 bax(-) and hct116 chk2(-) cells, administration of mk-8745 significantly inhibited tumor growth [3].

target

Aurora A

References

[1]. nair, j.s., a.l. ho, and g.k. schwartz, the induction of polyploidy or apoptosis by the aurora a kinase inhibitor mk8745 is p53-dependent. cell cycle, 2012. 11(4): p. 807-17.
[2]. chowdhury, a., s. chowdhury, and m.y. tsai, a novel aurora kinase a inhibitor mk-8745 predicts tpx2 as a therapeutic biomarker in non-hodgkin lymphoma cell lines. leuk lymphoma, 2012. 53(3): p. 462-71.
[3]. shionome, y., et al., integrity of p53 associated pathways determines induction of apoptosis of tumor cells resistant to aurora-a kinase inhibitors. plos one, 2013. 8(1): p. e55457.