Molecular Weight(MW): 428.92
AZD5363 potently inhibits all isoforms of Akt(Akt1/Akt2/Akt3) with IC50 of 3 nM/8 nM/8 nM in cell-free assays, similar to P70S6K/PKA and lower activity towards ROCK1/2. Phase 2.
Cited by 10 Publications
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G-H. Analysis of cells treated with AZD5363 (500 nM) for 24 hrs. G.Western analysis of whole cell lysates. H. Cells labeled with Annexin V-FITC for 6h were imaged. Individual points are average for replicates assessed in duplicate. Midlines are the average ± S.D. Student’s T-test.
Cancer Res, 2016, 76(16):4752-64.. AZD5363 purchased from Selleck.
Inhibition of PI3K and Akt by LY294002 and AZD5363 was confirmed by analyzing expression and activation status of the ribosomal protein S6 by Western blot analysis of PC-3 clone #14 cells treated with 0.5 or 5 uM AZD5363 (AZD) and 10 uM LY294002 (LY). Tubulin was used as a loading control.
Cell Commun Signal 2014 12(1), 61. AZD5363 purchased from Selleck.
LNCaP, LNCaP95, VCaP and 22Rv1 cells were transfected with control or pooled siRNA for AKT 1–3 isoforms for 36 hours. Cells were then further treated with 5 uM AZD5363 (B) for another 18 hours. Protein lysates were immunoblotted with AR (N-20), AR-V7, Pan-AKT, p-AKT(ser473) and β-Actin antibodies. Results were repeated in more than three independent experiments.
PLoS One 2014 9(10), e108780. AZD5363 purchased from Selleck.
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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|Description||AZD5363 potently inhibits all isoforms of Akt(Akt1/Akt2/Akt3) with IC50 of 3 nM/8 nM/8 nM in cell-free assays, similar to P70S6K/PKA and lower activity towards ROCK1/2. Phase 2.|
|Features||Moderate preclinical tolerability, and PD characteristics of an AKT inhibitor. Distinct profile from other AKT inhibitors in clinical development.|
AZD5363 is a potent Akt inhibitor with IC50 of 3 nM, 8 nM and 8 nM for Akt1, Akt2 and Akt3, respectively.  AZD5363 inhibits phosphorylation of AKT substrates in cells with a potency of approximately 0.3 to 0.8 μM. AZD5363 inhibits the proliferation of 41 of 182 solid and hematologic tumor cell lines with a potency of < 3 μM.  Activating mutations in PIK3CA, loss or inactivation of tumor suppressor PTEN, or HER2 amplification all are significantly predictive of responsiveness to AZD5363. Additionally, correlation is also seen between the RAS mutation status of cell lines and resistance to AZD5363. 
|In vivo||Oral dosing of AZD5363 (100, 300 mg/kg) to nude mice causes dose- and time-dependent reduction of PRAS40, GSK3β, and S6 phosphorylation in BT474c xenografts, reversible increases in blood glucose concentrations, and dose-dependent decreases in 2[18F]fluoro-2-deoxy-d-glucose (18F-FDG) uptake in U87-MG xenografts. Chronic oral dosing of AZD5363 (130, 200, and 300 mg/kg) causes dose-dependent growth inhibition of xenografts derived from various tumor types, including HER2+ breast cancer models that are resistant to trastuzumab. AZD5363 also significantly enhances the antitumor activity of docetaxel, lapatinib, and trastuzumab in breast cancer xenografts. |
Caliper Off-Chip Incubation Mobility Shift assay:The ability of AZD5363 and other compounds to inhibit the activity of AKT1, AKT2, and AKT3 is evaluated by the Caliper Off-Chip Incubation Mobility Shift assay. Active recombinant AKT1, AKT2, or AKT3 are incubated with a 5-FAM-labeled custom-synthesized peptide substrate together with increasing concentrations of inhibitor. Final reactions contained 1 to 3 nM AKT1, AKT2, or AKT3 enzymes; 1.5 mM peptide substrate; ATP at K m for each AKT isoform; 10 mM MgCl2, 4 mM DTT, 100 mM HEPES, and 0.015% Brij-35. The reactions are incubated at room temperature for 1 hour and stopped by the addition of buffer containing 100 mM HEPES, 0.015% Brij-35 solution, 0.1% coating reagent, 40 mM EDTA, and 5% DMSO. Plates are then analyzed using a Caliper LC3000, allowing for separation of peptide substrate and phosphorylated product by electrophoresis with subsequent detection and quantification of laser induced fluorescence.
|In vitro||DMSO||86 mg/mL (200.5 mM)|
* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02576444||Recruiting||Cancer||Yale University|Dana-Farber Cancer Institute|Vanderbilt-Ingram Cancer Center||November 2015||Phase 2|
|NCT02465060||Recruiting||Advanced Malignant Neoplasm|Lymphoma|Refractory Malignant Neoplasm|Solid Neoplasm||National Cancer Institute (NCI)||August 2015||Phase 2|
|NCT02664935||Recruiting||Non-Small Cell Lung Cancer|Carcinoma, Squamous Cell|Adenocarcinoma||University of Birmingham|Cancer Research UK|AstraZeneca|Pfizer|Experimental Cancer Medicine Centre Network||March 2015||Phase 2|
|NCT02449655||Recruiting||Advanced Gastric Adenocarcinoma||Samsung Medical Center||February 2015||Phase 2|
|NCT02451956||Recruiting||Advanced Gastric Cancer||Samsung Medical Center||January 2015||Phase 2|
|NCT02525068||Recruiting||Adenocarcinoma of the Prostate||Institute of Cancer Research, United Kingdom|Royal Marsden NHS Foundation Trust||December 2014||Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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