AZD5363 Chemical Properties

Melting point:

161-164°C

Density 

1.381

storage temp. 

Refrigerator

solubility 

DMSO (Slightly), Methanol (Slightly)

pka

13.93±0.50(Predicted)

form 

Solid

color 

Off-White to Pale Beige

AZD5363 Usage And Synthesis

Uses

AZD5363 is used in inhibiting the proliferation of certain tumor cell lines.

Biological Activity

azd5363 is a novel, potent phosphoinositide 3-kinase (pi3k)/akt pathway inhibitor with ic50 value of ~200nm. [1]azd5363 is proved to inhibit castrate resistant prostate cancer (crpc) progression. clusterin (clu) and autophagy will be induced which may work as cytoprotective responses which can affect the downstream pi3k/akt signaling. [2] azd5363 inhibits the growth of a lot of human tumor cells in a dose dependent manner. the mode of action could be monotherapy as well as in combination with her2 inhibitors in breast cancer models. [3] it is suggested to induce cell apoptosis by measuring the expression of parp cleavage, the activity of caspase 3, et al. [1]most importantly, azd5363 can target the pi3k/akt-pathway in vivo significantly, thus reducing the serum psa-levels and tumor volume, finally, it could postpone the progression to crpc.[1]

target

Akt

storage

Store at -20°C

References

[1] thomas c, crafter c, davies b, zoubeidi a, gleave me. azd5363, a novel akt inhibitor, delays prostate cancer progression. the journal of urology. may 2011. 185(4s): e292-293.
[2] kumano m, zhang f, shiota m, crafter c, davies b, zoubeidi a, gleave m. clusterin knockdown enhances antitumor activity of a novel akt inhibitor, azd5363, through inhibition of autophagy in prostate cancer. the journal of urology. may 21 2012. e392.
[3] davies br, greenwood h, dudley p, et al. preclinical pharmacology of azd5363, an inhibitor of akt: pharmacodynamics, antitumor activity, and correlation of monotherapy activity with genetic background. mol. cancer ther. arp 2012. 11: 873.

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