AZD5363

Short Summary : AKT inhibitor,pyrrolopyrimidine derived

Category : PI3K/Akt/mTOR Signaling|Akt

Purity : 0.98

CAS Number : 1143532-39-1

Formula : C21H25ClN6O2

Molecular Weight : 428.92

SMILE : C1CN(CCC1(C(=O)NC(CCO)C2=CC=C(C=C2)Cl)N)C3=NC=NC4=C3C=CN4

Solubility : >21.5mg/mL in DMSO

Storage : Store at -20°C

Description : 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]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.

Download datasheet