Capivasertib (AZD5363)

For research use only.

Catalog No.S8019

75 publications

Capivasertib (AZD5363) Chemical Structure

CAS No. 1143532-39-1

Capivasertib (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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Selleck's Capivasertib (AZD5363) has been cited by 75 publications

Purity & Quality Control

Choose Selective Akt Inhibitors

Biological Activity

Description Capivasertib (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.
Targets
Akt1 [1]
(Cell-free assay)
Akt2 [1]
(Cell-free assay)
Akt3 [1]
(Cell-free assay)
ROCK2 [1]
(Cell-free assay)
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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PC-3  M4XC[2Z2dmO2aX;uJGF{e2G7 MXuxNEDPxE1? MX:xNkBp NGGxXYRqdmS3Y3XzJIF2fG:yaHHnfS=> MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ3OEe0NEc,OjN{NUi3OFA9N2F-
LNCaP MU\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NYXLXGNOOC1zMECwJI5O Mmn0NE01KGR? M3;oWJJm\HWlZXSgUG5E[VBiY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNSCjbnSgeIlu\S2mZYDlcoRmdnRibXHucoVzyqB? NFi5c289[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{K1PFc1OCd-MkOyOVg4PDB:L3G+
DU145  NGXJN4JHfW6ldHnvckBCe3OjeR?= NEPUTHoxNjVxMT:xNEDPxE1? M1XS[lQ5KGh? M1r0OIRwf26{ZXf1cIF1\XNidHjlJJBpd3OyaH;yfYxifGmxbjDv[kBld3ewc4Ty[YFuKHCjdHj3ZZkheHKxdHXpcpMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ3OEe0NEc,OjN{NUi3OFA9N2F-
PC-3 MYLGeY5kfGmxbjDBd5NigQ>? NIPZVIIxNjVxMT:xNEDPxE1? M1;K[lQ5KGh? M3n1e4Rwf26{ZXf1cIF1\XNidHjlJJBpd3OyaH;yfYxifGmxbjDv[kBld3ewc4Ty[YFuKHCjdHj3ZZkheHKxdHXpcpMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ3OEe0NEc,OjN{NUi3OFA9N2F-
C4-2  NWm0[IxET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofoNVAxNTVyMECgcm0> NVLpeYVyPzJiaB?= MWjpcoNz\WG|ZYOgeIhmKG[{YXP0bY9vKG:oIHPlcIx{KHWwZHXy[49qdmdiY3XscEBl\WG2aB?= NHjnfW49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m2OlYzOSd-MkO5OlY3OjF:L3G+
LNCaP M1fwXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\BO|YyODBvNUCwNEBvVQ>? M16wclczKGh? Mnv6bY5kemWjc3XzJJRp\SCocnHjeIlwdiCxZjDj[YxteyC3bnTldodwcW6pIHPlcIwh\GWjdHi= MkLOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7Nk[2NlEoRjJ|OU[2OlIyRC:jPh?=
C4-2  M3\qOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jhVVEuOTByMECgcm0> Ml3YNE0{KGR? NYi1e|BRcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl4Nk[yNUc,OjN7Nk[2NlE9N2F-
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C4-2  NILDW2VHfW6ldHnvckBCe3OjeR?= NW\IdoFSPSEQvF2= Mn\QNE0zPCCq MlOxbY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJJRp\SCmaYP0ZYwhSUuWLYDheIh4[XliYnnvcYFzc2W{czDpcoNtfWSrbnegVHJCWzRyLDDlTWY1TSxiNFWtRnAyNCCvVF;SMEBidmRiUEewJHM3KGurbnHz[UBqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=> NX7COpZWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OlY3OjFpPkKzPVY3PjJzPD;hQi=>
LNCaP NVe0XWdzTnWwY4Tpc44hSXO|YYm= NUizZm52PSEQvF2= NWW1U2xoOC1{NDDo MlXCbY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJJRp\SCmaYP0ZYwhSUuWLYDheIh4[XliYnnvcYFzc2W{czDpcoNtfWSrbnegVHJCWzRyLDDlTWY1TSxiNFWtRnAyNCCvVF;SMEBidmRiUEewJHM3KGurbnHz[UBqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=> MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl4Nk[yNUc,OjN7Nk[2NlE9N2F-
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LNCaP MmW5SpVv[3Srb36gRZN{[Xl? M1vP[lUh|ryP NGKxNWUxNTJ2IHi= M{LxT4lv\HWlZYOgRWtVWzR5MzDhcoQhSUuWVEOwPEBxcG:|cHjvdplt[XSrb36gbY4h[SC2aX3lJIRmeGWwZHXueEBu[W6wZYK= MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl4Nk[yNUc,OjN7Nk[2NlE9N2F-
PAMC82 NX35eG5vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvXVGF7UUN3ME2zNEDPxE1? M4G1UVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEi4N|gzLz5{NEC4PFM5OjxxYU6=
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GTL-16 M1TrOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzqPWYzUUN3ME2zNEDPxE1? MnrEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyOEizPFIoRjJ2MEi4N|gzRC:jPh?=
SNU-5 NGTa[ppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDlTWM2OD1|MDFOwG0> MoTvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyOEizPFIoRjJ2MEi4N|gzRC:jPh?=
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PTEN-null LNCAP NHHkSoxHfW6ldHnvckBie3OjeR?= NELXUVUyKGi{ M1TafGlvcGmkaYTpc44hd2ZiQXv0JIlvKGi3bXHuJHBVTU5vboXscEBNVkODUDDj[YxteyCjc4Pld5Nm\CCjczDzeZBxemW|c3nvckBqdiCSUlHTOFAheGixc4Doc5J6dGG2aX;uJIFnfGW{IEGgbJIh[nliRVzJV2Eh[W6jbInzbZMtKEmFNUCgQUAxNjN|Nkig{txONg>? NYi4cZhFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewPFkzOTFpPkK3NFg6OjFzPD;hQi=>
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MG 63 (6-TG R) NFqxSplyUFSVIHHzd4F6 MmDhdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE2JIE[zJEg3NVSJIGKpJINmdGy| MnvrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pAKT / AKT / pGSK3β / GSK3β; 

PubMed: 26998062     


AZD5363 inhibited the phosphorylation of GSK3β, but increased the phosphorylation of AKT in a time-dependent manner in the (A) Hep-G2 cells. 

HER3 / pHER3 / HER2 / pHER2 / pPRAS40 / pS6 / p-4EBP1 / pFOXO / pERK / PARP / Cleaved PARP; 

PubMed: 26095475     


(A) BT474c or HCC1954 cells were treated for 24 h with increasing concentrations of AZD5363 ±0.3 μM or 1 μM AZD8931, respectively. Protein lysates were analysed by immunoblot with the indicated antibodies. Blots are representative of blots from 2–3 separate experiments. 

26998062 26095475
Immunofluorescence
p-Chk2 / γ-H2AX; 

PubMed: 29879757     


(C) Cells were treated with AZD1208 and AZD5363 alone or in combination for 5 days, and immunofluorescence analysis was subsequently performed. Confocal microscopy was used to observe the signals corresponding to p-Chk2 (red) and γ-H2AX (green). DAPI (blue) was used as a nuclear counterstain. CI, combination index. Scale bars=5 μm.

29879757
Growth inhibition assay
Cell viability; 

PubMed: 29879757     


Cells were seeded and cultured with increasing concentrations of AZD5363 and 1 μM AZD1208 every 3 days. The cells were cultured for 14 days until colonies formed and were then stained. The percentages of surviving cells were calculated by counting the number of colonies and are presented in a bar graph with standard error bars (n=3). a)p < 0.005. 

29879757
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]

Protocol

Kinase Assay:[1]
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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 Research: [2]
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  • 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.
    (Only for Reference)
Animal Research:[2]
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  • Animal Models: Female nude mice and male SCID mice with BT474c, U87MG, KPL-4, HCC-1187 xenografts.
  • Dosages: 130 mg/Kg - 300 mg/Kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 86 mg/mL (200.5 mM)
Water Insoluble
Ethanol 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 Information

Molecular Weight 428.92
Formula

C21H25ClN6O2

CAS No. 1143532-39-1
Storage powder
in solvent
Synonyms N/A
Smiles C1CN(CCC1(C(=O)NC(CCO)C2=CC=C(C=C2)Cl)N)C3=NC=NC4=C3C=CN4

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03310541 Active not recruiting Drug: AZD5363|Drug: Enzalutamide|Drug: Fulvestrant Breast Cancer|Prostate Cancer|Advanced Solid Tumors Memorial Sloan Kettering Cancer Center October 11 2017 Phase 1
NCT01992952 Active not recruiting Drug: AZD5363|Drug: Placebo|Drug: Fulvestrant Estrogen Receptor Positive Breast Cancer Velindre NHS Trust|AstraZeneca|Cenduit LLC|Covance|Cardiff and Vale University Health Board May 2014 Phase 1|Phase 2
NCT02338622 Completed Drug: olaparib|Drug: AZD5363 Advanced Cancer Royal Marsden NHS Foundation Trust|Institute of Cancer Research United Kingdom|AstraZeneca March 31 2014 Phase 1
NCT02121639 Active not recruiting Drug: Placebo|Drug: AZD5363 Prostate Cancer University Hospital Southampton NHS Foundation Trust|AstraZeneca|Cancer Research UK January 29 2014 Phase 1|Phase 2
NCT02077569 Completed Drug: AZD5363 Invasive Breast Cancer University of Nottingham|AstraZeneca|Cancer Research UK|National Cancer Research Network January 2014 Phase 2
NCT01692262 Completed Drug: Intermittent dosing of AZD5363 Metastatic Castrate-Resistant Prostate Cancer (mCRPC)|Efficacy|Safety and Tolerability|Pharmacokinetics|Pharmacodynamics|Tumour Response. AstraZeneca November 2012 Phase 1

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID