ホームページ PI3K/Akt/mTOR Akt inhibitor Capivasertib (AZD5363) For research use only.

Capivasertib (AZD5363)

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)化学構造

CAS No. 1143532-39-1

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 35200 国内在庫あり
JPY 22000 国内在庫あり
JPY 70500 国内在庫あり
JPY 175500 国内在庫あり
JPY 370500 国内在庫あり

代表番号: 045-509-1970|電子メール：[email protected]
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Capivasertib (AZD5363)関連製品

シグナル伝達経路

Akt Signaling Pathways

Aktシグナル伝達経路

Akt阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
LNCaP Function Assay 5 μM 0-24 h induces AKTS473 and AKTT308 phosphorylation in a time dependent manner 23966621
C4-2  Function Assay 5 μM 0-24 h induces AKTS473 and AKTT308 phosphorylation in a time dependent manner 23966621
LNCaP Function Assay 5 μM 0-24 h inhibits phosphorylation of the distal AKT-pathway biomarkers including PRAS40, eIF4E, 4E-BP1, mTOR, and P70 S6 kinase in a time-dependent manner 23966621
C4-2  Function Assay 5 μM 0-24 h inhibits phosphorylation of the distal AKT-pathway biomarkers including PRAS40, eIF4E, 4E-BP1, mTOR, and P70 S6 kinase in a time-dependent manner 23966621
LNCaP Growth Inhibition Assay 1-10000 nM 0-3 d inhibits cell viability dose dependently 23966621
C4-2  Growth Inhibition Assay 1-10000 nM 0-3 d inhibits cell viability dose dependently 23966621
LNCaP Growth Inhibition Assay 100-5000 nM 72 h increases the fraction of cells undergoing cell death 23966621
C4-2  Growth Inhibition Assay 100-5000 nM 72 h increases the fraction of cells undergoing cell death 23966621
PC-3 Function Assay 0.5/1/10 μM 48 h downregulates the phosphorylation of downstream pathway proteins in a dose-dependent manner 23258740
DU145  Function Assay 0.5/1/10 μM 48 h downregulates the phosphorylation of downstream pathway proteins in a dose-dependent manner 23258740
LNCaP Cell Viability Assay 0-1000 nM 0-4 d reduced LNCaP cell viability in a dose- and time-dependent manner  23258740
PC-3  Function Assay 10 μM 12 h induces autophagy 23258740
PC-9 Function Assay 1/5/10 μM 4/24 h increases AKT phosphorylation 24957682
NCI-H522 Function Assay 1/5/10 μM 4/24 h increases AKT phosphorylation 24957682
MR49F Growth Inhibition Assay 0-5 μM 48 h inhibits cell growth in a dose dependent manner 25151012
MR49C Growth Inhibition Assay 0-5 μM 48 h inhibits cell growth in a dose dependent manner 25151012
SKBR3 Growth Inhibition Assay 0-1.35 μM 5 d enhances the growth inhibition of AZD8931 26095475
KPL4 Growth Inhibition Assay 0-1.35 μM 5 d enhances the growth inhibition of AZD8931 26095475
BT474c Growth Inhibition Assay 0-1.35 μM 5 d enhances the growth inhibition of AZD8931 26095475
HCC1954 Growth Inhibition Assay 0-1.35 μM 5 d enhances the growth inhibition of AZD8931 26095475
TamR Growth Inhibition Assay 400 nM 6 d increased drug sensitivity of 4-OHT and fulvestrant 26351323
T74D LTED Growth Inhibition Assay 100 nM 6 d increased drug sensitivity of 4-OHT and fulvestrant 26351323
ZR75 LTED Growth Inhibition Assay 100 nM 6 d increased drug sensitivity of 4-OHT and fulvestrant 26351323
MCF7 LTED Growth Inhibition Assay 200 nM 6 d increased drug sensitivity of 4-OHT and fulvestrant 26351323
1%MCF7 Growth Inhibition Assay 400 nM 6 d increased drug sensitivity of 4-OHT and fulvestrant 26351323
T74D Growth Inhibition Assay 100 nM 6 d increased drug sensitivity of 4-OHT and fulvestrant 26351323
ZR75 Growth Inhibition Assay 100 nM 6 d increased drug sensitivity of 4-OHT and fulvestrant 26351323
MCF7 Growth Inhibition Assay 200 nM 6 d increased drug sensitivity of 4-OHT and fulvestrant 26351323
MDA-MB-468 Function assay 2 hrs Inhibition of Akt in human MDA-MB-468 cells assessed as inhibition of GSK3beta phosphorylation after 2 hrs by laser scanning cytometry, IC50 = 0.089 μM. 23394218
PTEN-null LNCAP Function assay 1 hr Inhibition of Akt in human PTEN-null LNCAP cells assessed as suppression in PRAS40 phosphorylation after 1 hr by ELISA analysis, IC50 = 0.3368 μM. 27089211
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay, IC50 = 5.2 μM. 27089211
OVCAR8 Antiproliferative assay 72 hrs Antiproliferative activity against human OVCAR8 cells after 72 hrs by SRB assay, IC50 = 7.27 μM. 27089211
SNU-638 Growth Inhibition Assay IC50=4.523 μM 24088382
SNU-1 Growth Inhibition Assay IC50=5.258 μM 24088382
SNU-601 Growth Inhibition Assay IC50=5.938 μM 24088382
SNU-668 Growth Inhibition Assay IC50=6.003 μM 24088382
HS746T Growth Inhibition Assay IC50=6.084 μM 24088382
KATO III Growth Inhibition Assay IC50=7.267 μM 24088382
SNU-484 Growth Inhibition Assay IC50=7.392 μM 24088382
OCUM-1 Growth Inhibition Assay IC50=14.515 μM 24088382
SNU-16 Growth Inhibition Assay IC50=11.097 μM 24088382
NUGC-3 Growth Inhibition Assay IC50=21.873 μM 24088382
AZ521 Growth Inhibition Assay IC50=25.448 μM 24088382
SNU-216 Growth Inhibition Assay IC50=30 μM 24088382
NUGC-4 Growth Inhibition Assay IC50=30 μM 24088382
SNU-5 Growth Inhibition Assay IC50=30 μM 24088382
GTL-16 Growth Inhibition Assay IC50=30 μM 24088382
MKN74 Growth Inhibition Assay IC50=30 μM 24088382
PAMC82 Growth Inhibition Assay IC50=30 μM 24088382
SNU-620 Growth Inhibition Assay IC50=3.384 μM 24088382
MKN1 Growth Inhibition Assay IC50=2.421 μM 24088382
23132/87 Growth Inhibition Assay IC50=1.671 μM 24088382
NCI-N87 Growth Inhibition Assay IC50=1.037 μM 24088382
AGS Growth Inhibition Assay IC50=0.552 μM 24088382
IM95m Growth Inhibition Assay IC50=0.51 μM 24088382
HGC27 Growth Inhibition Assay IC50=0.445 μM 24088382
PC-9 Growth Inhibition Assay IC50=9.3 (±1.2) μM 24957682
NCI-H522 Growth Inhibition Assay IC50=11.3 (±2.7) μM 24957682
LNCaP Function assay Inhibition of Akt in PTEN-deficient human LNCaP cells assessed as phosphorylation of GSK3beta, IC50 = 0.06 μM. 23394218
LNCaP Function assay Inhibition of Akt in PTEN-deficient human LNCaP cells assessed as phosphorylation of PRAS40, IC50 = 0.22 μM. 23394218
BT474c Function assay Inhibition of Akt in human BT474c cells harboring HER2+/PIK3CA double mutant assessed as phosphorylation of PRAS40, IC50 = 0.31 μM. 23394218
MDA-MB-468 Function assay Inhibition of Akt in PTEN-deficient human MDA-MB-468 cells assessed as phosphorylation of GSK3beta, IC50 = 0.38 μM. 23394218
MDA-MB-468 Function assay Inhibition of Akt in PTEN-deficient human MDA-MB-468 cells assessed as phosphorylation of PRAS40, IC50 = 0.39 μM. 23394218
BT474c Function assay Inhibition of Akt in human BT474c cells harboring HER2+/PIK3CA double mutant assessed as phosphorylation of GSK3beta, IC50 = 0.76 μM. 23394218
RT4 Function assay Inhibition of PKA in TSC1 deficient human RT4 cells assessed as S6 phosphorylation, IC50 = 1 μM. 23394218
RT4 Function assay Inhibition of P70S6K in TSC1 deficient human RT4 cells assessed as S6 phosphorylation, IC50 = 5 μM. 23394218
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
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生物活性

製品説明 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.
特性 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
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]
Kinase Assay 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.
細胞実験 細胞株 182 solid and hematologic tumor cell lines
濃度 ~30 μM
反応時間 72 hours
実験の流れ

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.
実験結果図 Methods Biomarkers 結果図 PMID
Western blot pAKT / AKT / pGSK3β / GSK3β HER3 / pHER3 / HER2 / pHER2 / pPRAS40 / pS6 / p-4EBP1 / pFOXO / pERK / PARP / Cleaved PARP 26998062
Immunofluorescence p-Chk2 / γ-H2AX 29879757
Growth inhibition assay Cell viability 29879757
In Vivo
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.
動物実験 動物モデル Female nude mice and male SCID mice with BT474c, U87MG, KPL-4, HCC-1187 xenografts.
投与量 130 mg/Kg - 300 mg/Kg
投与経路 p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03310541 Completed
Breast Cancer|Prostate Cancer|Advanced Solid Tumors
Memorial Sloan Kettering Cancer Center
 October 11 2017 Phase 1
NCT01992952 Active not recruiting
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
Advanced Cancer
Royal Marsden NHS Foundation Trust|Institute of Cancer Research United Kingdom|AstraZeneca
 March 31 2014 Phase 1
NCT02121639 Completed
Prostate Cancer
University Hospital Southampton NHS Foundation Trust|AstraZeneca|Cancer Research UK
 January 29 2014 Phase 1|Phase 2
NCT02077569 Completed
Invasive Breast Cancer
University of Nottingham|AstraZeneca|Cancer Research UK|National Cancer Research Network
 January 2014 Phase 2
NCT01692262 Completed
Metastatic Castrate-Resistant Prostate Cancer (mCRPC)|Efficacy|Safety and Tolerability|Pharmacokinetics|Pharmacodynamics|Tumour Response.
AstraZeneca
 November 2012 Phase 1

化学情報

分子量 428.92 化学式

C21H25ClN6O2
CAS No. 1143532-39-1 SDF Download Capivasertib (AZD5363) SDFをダウンロードする
Smiles C1CN(CCC1(C(=O)NC(CCO)C2=CC=C(C=C2)Cl)N)C3=NC=NC4=C3C=CN4
保管

In vitro
Batch:

DMSO : 86 mg/mL ( (200.5 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 30 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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