(2S)-1-[3-Ethyl-7-[[(1-oxido-3-pyridinyl)methyl]amino]pyrazolo[1,5-a]pyrimidin-5-yl]-2-piperidineethanol Chemical Properties

Melting point:

>78oC (dec.)

Density 

1.33

storage temp. 

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

solubility 

Chloroform (Slightly), Methanol (Slightly)

pka

15.15±0.10(Predicted)

form 

Solid

color 

White to Light Beige

Stability:

Hygroscopic

CAS DataBase Reference

779353-01-4

(2S)-1-[3-Ethyl-7-[[(1-oxido-3-pyridinyl)methyl]amino]pyrazolo[1,5-a]pyrimidin-5-yl]-2-piperidineethanol Usage And Synthesis

Uses

Dinaciclib is a potent and selective inhibitor of cyclin-dependent kinases which is undergoing development as oncology therapeutics.

Definition

ChEBI: 2-[(2S)-1-[3-ethyl-7-[(1-oxido-3-pyridin-1-iumyl)methylamino]-5-pyrazolo[1,5-a]pyrimidinyl]-2-piperidinyl]ethanol is a pyrazolopyrimidine.

Biological Activity

dinaciclib is a potent cyclin-dependent kinase (cdk) inhibitor with ic50s for cdk2, cdk5, cdk1 and cdk9 at 1 nm, 1 nm, 3 nm, and 4 nm, respectively. [1] it is in phase i or ii

target

CDK2

storage

Store at -20°C

References

[1]parry d., et al. (2010). dinaciclib (sch 727965), a novel and potent cyclin-dependent kinase inhibitor. mol cancer ther (9): 2344- 2353.
[2]martin, m. p., et al. (2013). cyclin-dependent kinase inhibitor dinaciclib interacts with the acetyl-lysine recognition site of bromodomains. acs chemical biology 8 (11): 2360–5.
[3]payton m., et al. (2006). discovery and evaluation of dual cdk1 and cdk2 inhibitors. cancer res 66: 4299-4308.

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