MK-5108 (VX-689) Property

Boiling point:

637.6±65.0 °C(Predicted)

Density 

1.429

storage temp. 

under inert gas (nitrogen or Argon) at 2–8 °C

solubility 

≥23.1 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O

form 

solid

pka

4.41±0.44(Predicted)

color 

White to 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.

MK-5108 (VX-689) Chemical Properties,Usage,Production

Uses

MK-5108 is a highly selective Aurora-A kinase inhibitor that shows antitumor activity alone and in combination with Docetaxel (D494420).

Definition

ChEBI: 4-(3-chloro-2-fluorophenoxy)-1-[[6-(2-thiazolylamino)-2-pyridinyl]methyl]-1-cyclohexanecarboxylic acid is an aromatic ether.

Biological Activity

mk-5108, also known as vx-689, is a novel, potent and selective inhibitor of aurora a kinase (aak) that competitively binds to the atp binding site of aak and hence potently inhibits the activity of aak with 50% inhibition concentration ic50 value of 0.064 nm. mk-5108 also inhibits other members of aurora kinase family, including aurora b kinase (ic50 = 14 nm) and aurora c kinase (ic50 = 12 nm), with a lesser potency. mk-5108 has been extensively studies and found to exhibit antitumor activity in a wide range of cancer types, including breast, cervix, colorectal, ovary and pancreas neoplasms.myke r. green, bs, pharm.d., bcop, joseph e. woolery, bs, pharm.d, and daruka mahadevan, md, phd. update on aurora kinase targeted therapeutics in oncology. recent pat anticancer drug discov. 2008 november ; 3(3): 162–177.

target

Aurora-A