Capivasertib (AZD5363)

Catalog No.S8019

For research use only.

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.

Capivasertib (AZD5363) Chemical Structure

CAS No. 1143532-39-1

Selleck's Capivasertib (AZD5363) has been cited by 103 publications

Purity & Quality Control

Choose Selective Akt Inhibitors

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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  MkLjSpVv[3Srb36gRZN{[Xl? NEjFRYcyOCEQvF2= MYmxNkBp M{PTdYlv\HWlZYOgZZV1d3CqYXf5 MnPFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{NUi3OFAoRjJ|MkW4O|QxRC:jPh?=
LNCaP M4nnUmNmdGxiVnnhZoltcXS7IFHzd4F6 M1TkW|AuOTByMDDuUS=> M1myUlAuPCCm NWLPOZR3emWmdXPl[EBNVkOjUDDj[YxtKH[rYXLpcIl1gSCrbjDhJIRwe2VvIHHu[EB1cW2nLXTldIVv\GWwdDDtZY5v\XMEoB?= MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ3OEe0NEc,OjN{NUi3OFA9N2F-
DU145  NV3WOmgyTnWwY4Tpc44hSXO|YYm= M17OdVAvPS9zL{GwJO69VQ>? MkjUOFghcA>? NHvH[lZld3ewcnXneYxifGW|IITo[UBxcG:|cHjvdplt[XSrb36gc4Yh\G:5boP0doVidSCyYYToe4F6KHC{b4TlbY5{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MmK3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{NUi3OFAoRjJ|MkW4O|QxRC:jPh?=
PC-3 NYLwNmw5TnWwY4Tpc44hSXO|YYm= MlXxNE42NzFxMUCg{txO MYG0PEBp M1XB[oRwf26{ZXf1cIF1\XNidHjlJJBpd3OyaH;yfYxifGmxbjDv[kBld3ewc4Ty[YFuKHCjdHj3ZZkheHKxdHXpcpMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MkiwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{NUi3OFAoRjJ|MkW4O|QxRC:jPh?=
C4-2  MmXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXtV3IzOTByLUWwNFAhdk1? MVO3NkBp MXHpcoNz\WG|ZYOgeIhmKG[{YXP0bY9vKG:oIHPlcIx{KHWwZHXy[49qdmdiY3XscEBl\WG2aB?= NV7iPJNrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OlY3OjFpPkKzPVY3PjJzPD;hQi=>
LNCaP MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXDbGQyODBvNUCwNEBvVQ>? NXTBWohGPzJiaB?= M{HXWIlv[3KnYYPld{B1cGViZoLhZ5Rqd25ib3[gZ4VtdHNidX7k[ZJod2mwZzDj[YxtKGSnYYTo NXfBbWtuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OlY3OjFpPkKzPVY3PjJzPD;hQi=>
C4-2  M3HzS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVGxMVExODByIH7N NHPSOZYxNTNiZB?= MYXpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl4Nk[yNUc,OjN7Nk[2NlE9N2F-
LNCaP NIfsfoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV2xMVExODByIH7N M3vZeVAuOyCm NUjTWXNWcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NXLJXmN7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OlY3OjFpPkKzPVY3PjJzPD;hQi=>
C4-2  MmDXSpVv[3Srb36gRZN{[Xl? MYK1JO69VQ>? M2rJO|AuOjRiaB?= MVjpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[geIhmKGSrc4ThcEBCU1RvcHH0bJdigSCkaX;tZZJs\XK|IHnuZ4x2\GmwZzDQVmFUPDBuIHXJSlRGNCB2RT3CVFEtKG2WT2KsJIFv\CCSN{CgV|Yhc2mwYYPlJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy NHXzR4Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m2OlYzOSd-MkO5OlY3OjF:L3G+
LNCaP NH3kenJHfW6ldHnvckBCe3OjeR?= NG\wPIc2KM7:TR?= MkPiNE0zPCCq MoDHbY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJJRp\SCmaYP0ZYwhSUuWLYDheIh4[XliYnnvcYFzc2W{czDpcoNtfWSrbnegVHJCWzRyLDDlTWY1TSxiNFWtRnAyNCCvVF;SMEBidmRiUEewJHM3KGurbnHz[UBqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=> M{PRfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OU[2OlIyLz5{M{m2OlYzOTxxYU6=
C4-2  NEGzUpFHfW6ldHnvckBCe3OjeR?= MVy1JO69VQ>? NHfQPGMxNTJ2IHi= M1ziZYlv\HWlZYOgRWtVWzR5MzDhcoQhSUuWVEOwPEBxcG:|cHjvdplt[XSrb36gbY4h[SC2aX3lJIRmeGWwZHXueEBu[W6wZYK= M2DVOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OU[2OlIyLz5{M{m2OlYzOTxxYU6=
LNCaP MWfGeY5kfGmxbjDBd5NigQ>? Mn3mOUDPxE1? NVXWfoVbOC1{NDDo M3G0Uolv\HWlZYOgRWtVWzR5MzDhcoQhSUuWVEOwPEBxcG:|cHjvdplt[XSrb36gbY4h[SC2aX3lJIRmeGWwZHXueEBu[W6wZYK= M3L6TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OU[2OlIyLz5{M{m2OlYzOTxxYU6=
PAMC82 MkW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHX1RplKSzVyPUOwJO69VQ>? MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB6OEO4Nkc,OjRyOEizPFI9N2F-
MKN74 MkfQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\rSWlEPTB;M{Cg{txO MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB6OEO4Nkc,OjRyOEizPFI9N2F-
GTL-16 NYDhVIRIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYW1fmVzUUN3ME2zNEDPxE1? MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB6OEO4Nkc,OjRyOEizPFI9N2F-
SNU-5 NULwUZNRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;ZPGlEPTB;M{Cg{txO MmqwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyOEizPFIoRjJ2MEi4N|gzRC:jPh?=
NUGC-4 M3HoZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TiSGlEPTB;M{Cg{txO MkfRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyOEizPFIoRjJ2MEi4N|gzRC:jPh?=
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NUGC-3 M1H2TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PZdWlEPTB;MkGuPFc{KM7:TR?= MkXuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyOEizPFIoRjJ2MEi4N|gzRC:jPh?=
OCUM-1 NUP6b4tPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjr[YxEUUN3ME2xOE42OTVizszN M1\6O|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEi4N|gzLz5{NEC4PFM5OjxxYU6=
SNU-16 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTw[oFKSzVyPUGxMlA6PyEQvF2= MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB6OEO4Nkc,OjRyOEizPFI9N2F-
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KATO III MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2THTGlEPTB;Nz6yOlch|ryP NF\HWmo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC4PFM5Oid-MkSwPFg{QDJ:L3G+
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SNU-601 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDRellKSzVyPUWuPVM5KM7:TR?= NUSxTnFzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPFg{QDJpPkK0NFg5Ozh{PD;hQi=>
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Assay
Methods Test Index PMID
Western blot pAKT / AKT / pGSK3β / GSK3β ; HER3 / pHER3 / HER2 / pHER2 / pPRAS40 / pS6 / p-4EBP1 / pFOXO / pERK / PARP / Cleaved PARP 26998062 26095475
Immunofluorescence p-Chk2 / γ-H2AX 29879757
Growth inhibition assay Cell viability 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 (from 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 Research: [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 Research:[2]
  • 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.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 428.92
Formula

C21H25ClN6O2

CAS No. 1143532-39-1
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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 Completed 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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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

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