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Submit ReviewAZD 5363 is a potent pan-AKT inhibitor (IC50 values are 3, 7 and 7 nM for AKt 1, 2 and 3, respectively). Also inhibits P70S6K, PKA, ROCK2 and ROCK1 (IC50 values are 6, 7, 60 and 470 nM, respectively). Inhibits growth of tumor cell lines in vitro, particularly breast, endometrial, gastric, hematologic and prostate cancers. Inhibits growth of human tumor xenografts in mice. Enhances in vivo antitumor effects of Docetaxel (Cat. No. 4056) and Lapatinib (Cat. No. 6811). Orally bioavailable.
AZD 5363 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
M. Wt | 428.92 |
Formula | C21H25ClN6O2 |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 1143532-39-1 |
PubChem ID | 25227436 |
InChI Key | JDUBGYFRJFOXQC-KRWDZBQOSA-N |
Smiles | NC1(CCN(CC1)C1=C2C=CNC2=NC=N1)C(=O)N[C@@H](CCO)C1=CC=C(Cl)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 42.89 | 100 |
The following data is based on the product molecular weight 428.92. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.33 mL | 11.66 mL | 23.31 mL |
5 mM | 0.47 mL | 2.33 mL | 4.66 mL |
10 mM | 0.23 mL | 1.17 mL | 2.33 mL |
50 mM | 0.05 mL | 0.23 mL | 0.47 mL |
References are publications that support the biological activity of the product.
Davies et al (2012) Preclinical pharmacology of AZD5363, an inhibitor of AKT: pharmacodynamics, antitumor activity, and correlation of monotherapy activity with genetic background. Mol.Cancer Ther. 11 873 PMID: 22294718
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