AZD5363

Catalog No.S8019

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.

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AZD5363 Chemical Structure

AZD5363 Chemical Structure
Molecular Weight: 428.92

Validation & Quality Control

2 customer reviews :

Quality Control & MSDS

Akt Inhibitors with Unique Features

  • Selective Akt Inhibitor

    CCT128930 Akt2-selective, IC50=6 nM.

  • Most Potent Akt Inhibitor

    GSK690693 Akt1, IC50=2 nM; Akt2, IC50=13 nM; Akt3, IC50=9 nM.

  • Akt Inhibitor in Clinical Trial

    Perifosine (KRX-0401) Phase III for relapsed and refractory multiple myeloma.

  • Classic Akt Inhibitor

    MK-2206 2HCl Highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, respectively; no inhibitory activities against 250 other protein kinases observed. Phase 2.

Product Information

  • Compare Akt Inhibitors
    Compare Akt Products
  • Research Area
  • Inhibition Profile

Product Description

Biological Activity

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.
Targets Akt1 [1]
(Cell-free assay)
Akt2 [1]
(Cell-free assay)
Akt3 [1]
(Cell-free assay)
ROCK2 [1]
(Cell-free assay)
IC50 3 nM 8 nM 8 nM 56 nM
In vitro AZD5363 is a potent Akt inhibitor with IC50 of 3 nM, 8 nM and 8 nM for Akt1, Akt2 and Akt3, respectively. [1] 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. [2] 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. [1]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
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PAMC82MlLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NVPQdZdxUUN3ME2zNEDPxE1?MV2yOFA5QDN6Mh?=
LNCaPNYDMN3BETnWwY4Tpc44hSXO|YYm=MVq1JO69VQ>?NXPmWWpXOC1{NDDoM1nJTYlv\HWlZYOgRWtVWzR5MzDhcoQhSUuWVEOwPEBxcG:|cHjvdplt[XSrb36gbY4h[SC2aX3lJIRmeGWwZHXueEBu[W6wZYK=NHfyW5QzOzl4Nk[yNS=>
C4-2 NWf6W4tOTnWwY4Tpc44hSXO|YYm=NIjiZY42KM7:TR?=M1XDU|AuOjRiaB?=MX;pcoR2[2W|IFHLWHM1PzNiYX7kJGFMXFR|MEigdIhwe3Cqb4L5cIF1cW:wIHnuJIEhfGmvZTDk[ZBmdmSnboSgcYFvdmW{M2XGbFI{QTZ4NkKx
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LNCaPMmrES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MlTYNU0yODByMDDuUS=>MoP1NE0{KGR?MVTpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6M2LoO|I{QTZ4NkKx
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LNCaPNELZRZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NFjENFQyODBvNUCwNEBvVQ>?M2j6XVczKGh?NXjWbY5tcW6lcnXhd4V{KHSqZTDmdoFkfGmxbjDv[kBk\WyuczD1coRmemexaX7nJINmdGxiZHXheIg>MYCyN|k3PjZ{MR?=
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PC-3 NIHMTIFHfW6ldHnvckBCe3OjeR?=MlviNVAh|ryPMo\PNVIhcA>?NXnwc3d4cW6mdXPld{BifXSxcHjh[5k>NGHGSmszOzJ3OEe0NC=>

... Click to View More Cell Line Experimental Data

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. [2]
Features Moderate preclinical tolerability, and PD characteristics of an AKT inhibitor. Distinct profile from other AKT inhibitors in clinical development.

Protocol(Only for Reference)

Kinase Assay: [1]

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.

Cell Assay: [2]

Cell lines 182 solid and hematologic tumor cell lines
Concentrations ~30 μM
Incubation Time 72 hours
Method Cell proliferation assay is determined by 2 methods, MTS and Sytox Green. Briefly, cells are seeded in 96-well plates and incubated overnight at 37 ℃, 5% CO2. Cells are then exposed to concentrations of AZD5363 ranging from 30 to 0.003μM for 72 hours. For the MTS endpoint, cell proliferation is measured by the CellTiter AQueous Non-Radioactive Cell Proliferation Assay reagent in accordance with the manufacturer's protocol. For the Sytox Green endpoint, Sytox Green nucleic acid dye diluted in TBS-EDTA buffer is added to cells (final concentration of 0.13 μM) and the number of dead cells detected using an Acumen Explorer. Cells are then permeabilized by the addition of saponin (0.03% final concentration, diluted in TBS-EDTA buffer), incubated overnight and a total cell count measured. Predose measurements are made for both MTS and Sytox Green endpoints, and concentration needed to reduce the growth of treated cells to half that of untreated cells values are determined using absorbance readings (MTS) or live cell counts.

Animal Study: [2]

Animal Models Female nude mice and male SCID mice with BT474c, U87MG, KPL-4, HCC-1187 xenografts.
Formulation In 10% DMSO 25% w/v Kleptose HPB
Dosages 130 mg/Kg - 300 mg/Kg
Administration p.o.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Addie M, et al. J Med Chem, 2013, 26.

[2] Davies BR, et al. Mol Cancer Ther, 2012, 11(4), 873-887.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-23)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02576444 Recruiting Cancer Yale University|Dana-Farber Cancer Institute|Vanderbilt-I  ...more 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|P  ...more 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

view more

Chemical Information

Download AZD5363 SDF Download AZD5363 SDF Download AZD5363 SDF
Molecular Weight (MW) 428.92
Formula

C21H25ClN6O2

CAS No. 1143532-39-1
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 86 mg/mL (200.5 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 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.
Chemical Name 4-Piperidinecarboxamide, 4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-

Customer Product Validation(2)


Click to enlarge
Rating
Source Cell Commun Signal 2014 12(1), 61. AZD5363 purchased from Selleck
Method Western blot
Cell Lines PC-3 clone #14 cells
Concentrations 0.5, 5 uM
Incubation Time
Results Since AZD5363 inhibits Akt without changing its phosphorylation level, it used phosphorylation of the downstream target, S6 ribosomal protein, to confirm that Akt and PI3K activity was suppressed by AZD5363 and LY294002.

Click to enlarge
Rating
Source PLoS One 2014 9(10), e108780. AZD5363 purchased from Selleck
Method Western blot
Cell Lines LNCaP, LNCaP95, VCaP, 22Rv1 cells
Concentrations 5 uM
Incubation Time 18 h
Results It observed that AZD5363 significantly increased AR-FL expressions in LNCaP and LNCaP95 cells and decreased AR-FL and AR-V7 in VCaP and 22Rv1 cells, which effects remained unchanged even in the presence of efficient AKT knockdown.

Tech Support

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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    AT13148 is an oral, ATP-competitive, multi-AGC kinase inhibitor with IC50 of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively. Phase 1.

  • SC79

    SC79 is a brain-penetrable Akt phosphorylation activator and an inhibitor of Akt-PH domain translocation.

  • MK-2206 2HCl

    MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM in cell-free assays, respectively; no inhibitory activities against 250 other protein kinases observed. Phase 2.

    Features:The first allosteric small molecule inhibitor of Akt to enter clinical development.

  • Ipatasertib (GDC-0068)

    Ipatasertib (GDC-0068) is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM in cell-free assays, 620-fold selectivity over PKA. Phase 2.

  • GSK690693

    GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. Phase 1.

  • Perifosine (KRX-0401)

    Perifosine (KRX-0401) is a novel Akt inhibitor with IC50 of 4.7 μM in MM.1S cells, targets pleckstrin homology domain of Akt. Phase 3.

  • A-674563

    A-674563 is an Akt1 inhibitor with Ki of 11 nM in cell-free assays, modest potent to PKA and >30-fold selective for Akt1 over PKC.

    Features:Orally bioavailable compound (achieved by replacing indole of A-443654 with phenyl moiety) and somewhat less selective for Akt over PKA than A-443654.

  • Triciribine

    Triciribine is a DNA synthesis inhibitor, also inhibits Akt in PC3 cell line and HIV-1 in CEM-SS, H9, H9IIIB, U1 cells with IC50 of 130 nM and 20 nM, respectively; does not inhibit PI3K/PDK1; 5000-fold less active in cells lacking adenosine kinase. Phase 1/2.

  • Honokiol

    Honokiol is the active principle of magnolia extract that inhibits Akt-phosphorylation and promotes ERK1/2 phosphorylation. Phase 3.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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