Cat. No.: HY-15431

Capivasertib

(Synonyms: AZD5363)

89 Cited Publications

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Based on 89 publication(s) in Google Scholar

Capivasertib (AZD5363) is an orally active and potent pan-AKT kinase inhibitor with IC₅₀ of 3, 7 and 7 nM for Akt1,Akt2 and Akt3, respectively.

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

Pureté: 99.96%
CAS No.: 1143532-39-1
Formule: C₂₁H₂₅ClN₆O₂
Masse moléculaire:428.92

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Capivasertib Chemical Structure

CAS No.: 1143532-39-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (89)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Capivasertib (AZD5363) is an orally active and potent pan-AKT kinase inhibitor with IC₅₀ of 3, 7 and 7 nM for Akt1,Akt2 and Akt3, respectively.

IC₅₀ & Target^[1]

Akt1

3 nM (IC₅₀)

Akt2

7 nM (IC₅₀)

Akt3

7 nM (IC₅₀)

P70S6K

6 nM (IC₅₀)

PKA

7 nM (IC₅₀)

ROCK2

60 nM (IC₅₀)

ROCK1

470 nM (IC₅₀)

Autophagy

Voir tous les produits spécifiques à Isoform Akt :

Cellular Effect

Cell Line	Type	Value	Description	References
769-P	IC₅₀	10.75 μM Compound: AZD5363	Antiproliferative activity against human 769-P cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human 769-P cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
786-0	IC₅₀	23.28 μM Compound: AZD5363	Antiproliferative activity against human 786-0 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human 786-0 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
A549	IC₅₀	23.67 μM Compound: AZD5363	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
AGS	IC₅₀	9.6 μM Compound: AZD5363	Antiproliferative activity against human AGS cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human AGS cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 34917257]
AN3-CA	EC₅₀	869 nM Compound: Capivasertib	Antiproliferative activity against human AN3-CA cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay Antiproliferative activity against human AN3-CA cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay	[PMID: 30996949]
AN3-CA	EC₅₀	869 nM Compound: Capivasertib	Antiproliferative activity against human AN3-CA cells assessed as reduction of cell growth measured after 5 days by CellTiter-Glo assay Antiproliferative activity against human AN3-CA cells assessed as reduction of cell growth measured after 5 days by CellTiter-Glo assay	[PMID: 31584233]
Bel-7402	IC₅₀	49.6 μM Compound: AZD5363	Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
BT-474	EC₅₀	1605 nM Compound: Capivasertib	Antiproliferative activity against human BT-474 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay Antiproliferative activity against human BT-474 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay	[PMID: 30996949]
CHO	IC₅₀	>100000 nM Compound: 64, AZD5363	Inhibition of human ERG expressed in CHO cells by ionworks assay Inhibition of human ERG expressed in CHO cells by ionworks assay	[PMID: 23394218]
HaCaT	IC₅₀	4.2 μM Compound: AZD5363	Antiproliferative activity against human HaCaT cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human HaCaT cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 34375113]
HCT-116	IC₅₀	5.2 μM Compound: AZD5363	Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay	[PMID: 27089211]
HCT-116	IC₅₀	5.2 μM Compound: AZD5363	Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay	[PMID: 31298542]
HepG2	IC₅₀	6.7 μM Compound: AZD5363	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
HT-29	IC₅₀	36.92 μM Compound: AZD5363	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
KHOS/NP	IC₅₀	40.42 μM Compound: AZD5363	Antiproliferative activity against human KHOS cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human KHOS cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
KU-19-19	EC₅₀	20866 nM Compound: Capivasertib	Antiproliferative activity against human KU-19-19 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay Antiproliferative activity against human KU-19-19 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay	[PMID: 30996949]
LNCaP	IC₅₀	0.06 μM Compound: 64, AZD5363	Inhibition of Akt in PTEN-deficient human LNCaP cells assessed as phosphorylation of GSK3beta Inhibition of Akt in PTEN-deficient human LNCaP cells assessed as phosphorylation of GSK3beta	[PMID: 23394218]
LNCaP	IC₅₀	0.22 μM Compound: 64, AZD5363	Inhibition of Akt in PTEN-deficient human LNCaP cells assessed as phosphorylation of PRAS40 Inhibition of Akt in PTEN-deficient human LNCaP cells assessed as phosphorylation of PRAS40	[PMID: 23394218]
LNCaP	IC₅₀	336.8 nM Compound: AZD5363	Inhibition of Akt in human PTEN-null LNCAP cells assessed as suppression in PRAS40 phosphorylation after 1 hr by ELISA analysis Inhibition of Akt in human PTEN-null LNCAP cells assessed as suppression in PRAS40 phosphorylation after 1 hr by ELISA analysis	[PMID: 27089211]
LNCaP	IC₅₀	0.178 μM Compound: AZD5363	Antiproliferative activity against human LNCAP cells Antiproliferative activity against human LNCAP cells	[PMID: 31298542]
LNCaP	IC₅₀	0.46 μM Compound: AZD5363	Antiproliferative activity against human LNCaP cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human LNCaP cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
MCF7	EC₅₀	555 nM Compound: Capivasertib	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay	[PMID: 30996949]
MCF7	IC₅₀	4.2 μM Compound: AZD5363	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 34917257]
MDA-MB-231	IC₅₀	60.52 μM Compound: AZD5363	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
MDA-MB-231	IC₅₀	3 nM Compound: AZD5363	Inhibition of AKT phosphorylation in human MDA-MB-231 incubated for 18 hrs by Western blot analysis Inhibition of AKT phosphorylation in human MDA-MB-231 incubated for 18 hrs by Western blot analysis	[PMID: 38592948]
MDA-MB-468	IC₅₀	0.38 μM Compound: 64, AZD5363	Inhibition of Akt in PTEN-deficient human MDA-MB-468 cells assessed as phosphorylation of GSK3beta Inhibition of Akt in PTEN-deficient human MDA-MB-468 cells assessed as phosphorylation of GSK3beta	[PMID: 23394218]
MDA-MB-468	IC₅₀	0.39 μM Compound: 64, AZD5363	Inhibition of Akt in PTEN-deficient human MDA-MB-468 cells assessed as phosphorylation of PRAS40 Inhibition of Akt in PTEN-deficient human MDA-MB-468 cells assessed as phosphorylation of PRAS40	[PMID: 23394218]
MDA-MB-468	IC₅₀	89 nM Compound: 64, AZD5363	Inhibition of Akt in human MDA-MB-468 cells assessed as inhibition of GSK3beta phosphorylation after 2 hrs by laser scanning cytometry Inhibition of Akt in human MDA-MB-468 cells assessed as inhibition of GSK3beta phosphorylation after 2 hrs by laser scanning cytometry	[PMID: 23394218]
MDA-MB-468	GI₅₀	3.8 μM Compound: AZD5363	Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth by measured after 5 days by IncuCyte zoom live cell analysis Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth by measured after 5 days by IncuCyte zoom live cell analysis	[PMID: 35119851]
NCI-H1975	IC₅₀	8.23 μM Compound: AZD5363	Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
NCI-H1975	IC₅₀	2.7 μM Compound: AZD5363	Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 34917257]
OS-RC-2	IC₅₀	53.43 μM Compound: AZD5363	Antiproliferative activity against human OS-RC-2 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human OS-RC-2 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
OVCAR-8	IC₅₀	7.27 μM Compound: AZD5363	Antiproliferative activity against human OVCAR8 cells after 72 hrs by SRB assay Antiproliferative activity against human OVCAR8 cells after 72 hrs by SRB assay	[PMID: 27089211]
OVCAR-8	IC₅₀	7.27 μM Compound: AZD5363	Antiproliferative activity against human OVCAR8 cells Antiproliferative activity against human OVCAR8 cells	[PMID: 31298542]
OVCAR-8	IC₅₀	4.48 μM Compound: AZD5363	Antiproliferative activity against human OVCAR-8 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human OVCAR-8 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
PC-3	IC₅₀	82.57 μM Compound: AZD5363	Antiproliferative activity against human PC3 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human PC3 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
PC-3	GI₅₀	6.5 μM Compound: AZD5363	Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth measured after 5 days by IncuCyte zoom live cell analysis Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth measured after 5 days by IncuCyte zoom live cell analysis	[PMID: 35119851]
RT-4	IC₅₀	1 μM Compound: 64, AZD5363	Inhibition of PKA in TSC1 deficient human RT4 cells assessed as S6 phosphorylation Inhibition of PKA in TSC1 deficient human RT4 cells assessed as S6 phosphorylation	[PMID: 23394218]
RT-4	IC₅₀	5 μM Compound: 64, AZD5363	Inhibition of P70S6K in TSC1 deficient human RT4 cells assessed as S6 phosphorylation Inhibition of P70S6K in TSC1 deficient human RT4 cells assessed as S6 phosphorylation	[PMID: 23394218]
SK-OV-3	IC₅₀	6.32 μM Compound: AZD5363	Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
SMMC-7721	IC₅₀	84.12 μM Compound: AZD5363	Antiproliferative activity against human SMMC-7721 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human SMMC-7721 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
T47D	EC₅₀	475 nM Compound: Capivasertib	Antiproliferative activity against human T47D cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay Antiproliferative activity against human T47D cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay	[PMID: 30996949]
T47D	EC₅₀	475 nM Compound: Capivasertib	Antiproliferative activity against human T47D cells assessed as reduction of cell growth measured after 5 days by CellTiter-Glo assay Antiproliferative activity against human T47D cells assessed as reduction of cell growth measured after 5 days by CellTiter-Glo assay	[PMID: 31584233]
U-251	IC₅₀	14.22 μM Compound: AZD5363	Antiproliferative activity against human U251 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human U251 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
U-87MG ATCC	IC₅₀	50.6 μM Compound: AZD5363	Antiproliferative activity against human U-87MG cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method Antiproliferative activity against human U-87MG cells assessed as inhibition of cell growth incubated for 72 hrs by SRB method	[PMID: 34375113]
Vero	CC₅₀	82 μM Compound: Capivasertib	Cytotoxicity in African green monkey Vero cells by MTT assay Cytotoxicity in African green monkey Vero cells by MTT assay	[PMID: 36857133]
ZR-75-1	EC₅₀	191 nM Compound: Capivasertib	Antiproliferative activity against human ZR-75-1 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay Antiproliferative activity against human ZR-75-1 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay	[PMID: 30996949]
ZR-75-1	EC₅₀	191 nM Compound: Capivasertib	Antiproliferative activity against human ZR-75-1 cells assessed as reduction of cell growth measured after 5 days by CellTiter-Glo assay Antiproliferative activity against human ZR-75-1 cells assessed as reduction of cell growth measured after 5 days by CellTiter-Glo assay	[PMID: 31584233]

In Vitro

Capivasertib, a novel pyrrolopyrimidine-derived compound, inhibits all AKT isoforms with a potency of 10 nM or less. Capivasertib inhibits phosphorylation of these substrates with an IC₅₀ value of 0.06 to 0.76 μM in the 3 cell lines. Capivasertib effectively inhibits phosphorylation of S6 and 4E-BP1 in these cell lines, whereas it increases phosphorylation of AKT at both ser⁴⁷³ and thr³⁰⁸. In BT474c cells, Capivasertib induces FOXO3a nuclear translocation with EC₅₀ value of 0.69 μM; a concentration of 3 μM is sufficient to almost completely localize FOXO3a to the nucleus. AZD5363Capivasertibhibitor MK-2206 is much less active (IC₅₀>30 μM)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Oral dosing of Capivasertib (AZD5363) to nude mice causes dose- and time-dependent reduction of PRAS40, GSK3β, and S6 phosphorylation in BT474c xenografts (PRAS40 phosphorylation EC₅₀ ~0.1 μM total plasma exposure), 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 Capivasertib caused dose-dependent growth inhibition of xenografts derived from various tumor types, including HER2⁺ breast cancer models. Capivasertib also significantly enhances the antitumor activity of RP-56976 and GW572016 in breast cancer xenografts^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1143532-39-1
Appearance Solid
Masse moléculaire 428.92
Formule C₂₁H₂₅ClN₆O₂
Color Off-white to gray
SMILES

O=C(C1(N)CCN(C2=C3C(NC=C3)=NC=N2)CC1)N[C@H](C4=CC=C(Cl)C=C4)CCO
Synonyms

AZD5363
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (89)

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Journal Impact Factor

Cell

RNA Pol II inhibition activates cell death independently from the loss of transcription. [Abstract]

2025 Oct 30;188(22):6301-6316.e29. PMID: 40818455
Exploration

Ion cocktail therapy for myocardial infarction by synergistic regulation of both structural and electrical remodeling. [Abstract]

2023 Nov 23;4(3):20230067. PMID: 38939858
Nat Aging

Shear stress governs hematopoietic stem cell fate to promote inflammation-induced aging. [Abstract]

2026 Jan 2. PMID: 41482519
Cancer Res

Blocking the TCA Cycle in Cancer Cells Potentiates CD36+ T-cell-Mediated Antitumor Immunity by Suppressing ER Stress-Associated THBS2 Signaling. [Abstract]

2025 Apr 28:OF1-OF13. PMID: 40293258
Cancer Res

GOT2 Silencing Promotes Reprogramming of Glutamine Metabolism and Sensitizes Hepatocellular Carcinoma to Glutaminase Inhibitors. [Abstract]

2022 Sep 16;82(18):3223-3235. PMID: 35895805
Cancer Res

Combinatorial Inactivation of Tumor Suppressors Efficiently Initiates Lung Adenocarcinoma with Therapeutic Vulnerabilities. [Abstract]

2022 Apr 15;82(8):1589-1602. PMID: 35425962
Cancer Res

Genomic Alterations in PIK3CA-Mutated Breast Cancer Result in mTORC1 Activation and Limit the Sensitivity to PI3Kα Inhibitors. [Abstract]

2021 May 1;81(9):2470-2480. PMID: 33685991
Nat Commun

Co-targeting CDK4/6 and AKT with endocrine therapy prevents progression in CDK4/6 inhibitor and endocrine therapy-resistant breast cancer. [Abstract]

2021 Aug 25;12(1):5112. PMID: 34433817

Capivasertib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Aug 25;12(1):5112. [Abstract]

The effect of AKT inhibitor (AKTi, capivasertib, 500 nM in the MCF-7 cell model) and CellTiter-Blue viabilityassay performed over 6 days.
Nat Commun

PLK1 inhibition exhibits strong anti-tumoral activity in CCND1-driven breast cancer metastases with acquired palbociclib resistance. [Abstract]

2020 Aug 13;11(1):4053. PMID: 32792481
Cell Death Differ

RIPK3 sequentially recruits MLKL and RIPK1 to induce PANoptosis and chemokine production. [Abstract]

2026 Apr 4. PMID: 41935203
Neuron

C5aR1+ microglia exacerbate neuroinflammation and cerebral edema in acute brain injury. [Abstract]

2025 Nov 18:S0896-6273(25)00803-7. PMID: 41260217
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Autophagy

The anti-cancer drug ABTL0812 induces ER stress-mediated cytotoxic autophagy by increasing dihydroceramide levels in cancer cells. [Abstract]

2021 Jun;17(6):1349-1366. PMID: 32397857
Adv Sci (Weinh)

AKT1 Phosphorylates FDX1 to Promote Cuproptosis Resistance in Triple-Negative Breast Cancer. [Abstract]

2025 Feb 20:e2408106. PMID: 39976173
Adv Sci (Weinh)

Targeting FDFT1 Reduces Cholesterol and Bile Acid Production and Delays Hepatocellular Carcinoma Progression Through the HNF4A/ALDOB/AKT1 Axis. [Abstract]

2025 Feb 3:e2411719. PMID: 39899681

Capivasertib purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Feb 3:e2411719. [Abstract]

Mice were treated with AZD5363 (100 mg/kg, once daily) by oral gavage. Representative images of pAKT1 (Ser473) (upper panel) and Ki67 (lower panel) staining of subcutaneous xenograft tumors were shown.
Neuro Oncol

Invasive growth of brain metastases is linked to CHI3L1 release from pSTAT3-positive astrocytes. [Abstract]

2024 Jun 3;26(6):1052-1066. PMID: 38271182

Capivasertib purchased from MedChemExpress. Usage Cited in: Neuro Oncol. 2024 Jun 3;26(6):1052-1066. [Abstract]

Immunoblot of PC9 cell signaling response to 24 h treatment with indicated concentrations of Capivasertib (0, 0.1, 0.5, 1, 5, 10, 25, 50, 100 μM) showed a dose-dependent decrease in phosphorylated AKT levels.
Cell Discov

ASCT2 palmitoylation regulated by JNK1-ZDHHC14 axis orchestrates glutamine metabolism and NSCLC progression. [Abstract]

2026 Feb 24;12(1):13. PMID: 41730846
Sci Adv

Epinephrine promotes breast cancer metastasis through a ubiquitin-specific peptidase 22-mediated lipolysis circuit. [Abstract]

2024 Aug 16;10(33):eado1533. PMID: 39151008
Carbohydr Polym

A novel strategy with in vivo characterization, extraction, isolation and activity evaluation for discovery of absorbed anti-inflammatory oligosaccharides from Zhu-Ling decoction. [Abstract]

2024 Oct 15:342:122422. PMID: 39048245
Redox Biol

DNAJC12 causes breast cancer chemotherapy resistance by repressing doxorubicin-induced ferroptosis and apoptosis via activation of AKT. [Abstract]

2024 Apr:70:103035. PMID: 38306757
Engineering

28 October 2022.

Capivasertib purchased from MedChemExpress. Usage Cited in: Engineering. 28 October 2022.

Lipid accumulation in adipocytes after the inhibition of Akt activity with capivasertib (Capi) (5 μM, six days) was measured with oil red O staining.
J Exp Med

EML4-ALK fusions drive lung adeno-to-squamous transition through JAK-STAT activation. [Abstract]

2024 Mar 4;221(3):e20232028. PMID: 38284990

Capivasertib purchased from MedChemExpress. Usage Cited in: J Exp Med. 2024 Mar 4;221(3):e20232028. [Abstract]

Western blot analyses of Club cell-derived EML4-ALK L1196M tumoroids were treated with indicated doses of capivasertib (Cap) (0, 1, 10, 100, 1000, 10000 nM) for 12 h and then subjected to western blot analyses.
Pharmacol Res

Fibroblast growth factor 18 exerts anti-osteoarthritic effects through PI3K-AKT signaling and mitochondrial fusion and fission. [Abstract]

2019 Jan:139:314-324. PMID: 30273654
Cancer Lett

Combined inhibition of CDK4/6 and AKT is highly effective against the luminal androgen receptor (LAR) subtype of triple negative breast cancer. [Abstract]

2024 Sep 5:217219. PMID: 39244005
Cell Death Dis

LIF is essential for ISC function and protects against radiation-induced gastrointestinal syndrome. [Abstract]

2020 Jul 27;11(7):588. PMID: 32719388
Int J Biol Macromol

Acetylation of GPRC5A at Lys348 facilitates cisplatin resistance and promotes the recurrence and poor prognosis in ovarian cancer. [Abstract]

2026 May:362:152113. PMID: 42009151
Acta Pharmacol Sin

Trimetazidine enhances myocardial angiogenesis in pressure overload-induced cardiac hypertrophy mice through directly activating Akt and promoting the binding of HSF1 to VEGF-A promoter. [Abstract]

2022 Oct;43(10):2550-2561. PMID: 35217815
EMBO J

Accelerated plasma-cell differentiation in Bach2-deficient mouse B cells is caused by altered IRF4 functions. [Abstract]

2024 May;43(10):1947-1964. PMID: 38605225
Phytomedicine

Atractylenolide I inhibits colorectal cancer cell proliferation by affecting metabolism and stemness via AKT/mTOR signaling. [Abstract]

2020 Mar;68:153191. PMID: 32135457
EMBO Mol Med

Epigenetic silencing of SALL2 confers tamoxifen resistance in breast cancer. [Abstract]

2019 Dec;11(12):e10638. PMID: 31657150
Biomed Pharmacother

MTMR14 protects against hepatic ischemia-reperfusion injury through interacting with AKT signaling in vivo and in vitro. [Abstract]

2020 Sep;129:110455. PMID: 32768948
Cell Mol Gastroenterol Hepatol

Fibrinogen/AKT/Microfilament Axis Promotes Colitis by Enhancing Vascular Permeability. [Abstract]

2021;11(3):683-696. PMID: 33075564
Oncogene

Olfactomedin 4 orchestrates TGF-β/CEACAM6 axis, promoting cell-autonomous epithelial to mesenchymal transition during gallbladder epithelium carcinogenesis. [Abstract]

2026 Jul;45(24):2359-2374. PMID: 42050078
Oncogene

Identification of RAPGEF3 as the therapeutic vulnerability of basal-subtype lung squamous cell carcinoma. [Abstract]

2025 Sep;44(34):3142-3148. PMID: 40781157
Oncogene

Fibroblast Activation Protein (FAP)+ cancer-associated fibroblasts induce macrophage M2-like polarization via the Fibronectin 1-Integrin α5β1 axis in breast cancer. [Abstract]

2025 Jul;44(28):2396-2412. PMID: 40263422
Cell Death Discov

Non-enzymatic function of QSOX2 directly regulates the JUNB-ITGB4 axis and enhanced resistance to osimertinib in EGFR-mutation lung adenocarcinoma. [Abstract]

2026 Apr 1;12(1):215. PMID: 41922310
Cell Rep

Biased signaling by mutant EGFR underlies dependence on PKCα in lung adenocarcinoma. [Abstract]

2024 Dec 3;43(12):115026. PMID: 39630579
Oncoimmunology

Ex vivo AKT-inhibition facilitates generation of polyfunctional stem cell memory-like CD8+ T cells for adoptive immunotherapy. [Abstract]

2018 Aug 6;7(10):e1488565. PMID: 30288356
EMBO Rep

IGF1R regulates retrograde axonal transport of signalling endosomes in motor neurons. [Abstract]

2020 Mar 4;21(3):e49129. PMID: 32030864
Food Biosci

April 2022, 101571.
J Invest Dermatol

Inhibition of the Extracellular Signal-Regulated Kinase/Ribosomal S6 Kinase Cascade Limits Chlamydia trachomatis Infection. [Abstract]

2021 Apr;141(4):852-862.e6. PMID: 32918951
Breast Cancer Res

MiR-4649-5p acts as a tumor-suppressive microRNA in triple negative breast cancer by direct interaction with PIP5K1C, thereby potentiating growth-inhibitory effects of the AKT inhibitor capivasertib. [Abstract]

2023 Oct 6;25(1):119. PMID: 37803350
Gastric Cancer

COPS5 inhibition synergizes with the antitumor effect of trastuzumab by PTEN upregulation in HER2-amplified gastric cancer. [Abstract]

2025 Oct 2. PMID: 41039054
Drug Des Devel Ther

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PLoS Pathog

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2024 Sep 3;20(9):e1012483. PMID: 39226326
Int J Mol Sci

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2024 May 17;25(10):5475. PMID: 38791513
Eur J Pharmacol

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2025 Nov 5:1006:178178. PMID: 40973011
Invest Ophthalmol Vis Sci

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2025 Apr 1;66(4):83. PMID: 40305469
Mol Cancer Res

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2019 Jul;17(7):1582-1593. PMID: 30975706
Mol Oncol

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2023 Nov;17(11):2451-2471. PMID: 37753805
Biochim Biophys Acta Mol Basis Dis

PI3K/Akt inhibition promotes AR activity and prostate cancer cell proliferation through p35-CDK5 modulation. [Abstract]

2024 Nov 11:167568. PMID: 39536992
Sci Rep

Analysis of capivasertib via ion-pairing with erythrocin B as a spectrofluorometric probe. [Abstract]

2026 May 1;16(1):14019. PMID: 42067575
Sci Rep

MiR-485-3p/MELK cascade mediates tumor progression in pancreatic cancer. [Abstract]

2025 May 22;15(1):17870. PMID: 40404813
Oncol Rep

Aprepitant inhibits the progression of esophageal squamous cancer by blocking the truncated neurokinin‑1 receptor. [Abstract]

2023 Jul;50(1):131. PMID: 37203393
Biomedicines

TIRAP/Mal Positively Regulates TLR8-Mediated Signaling via IRF5 in Human Cells. [Abstract]

2022 Jun 22;10(7):1476. PMID: 35884781
J Biol Chem

G protein βγ translocation to the Golgi apparatus activates MAPK via p110γ-p101 heterodimers. [Abstract]

2021 Jan-Jun:296:100325. PMID: 33493514
Aging (Albany NY)

Hsa_circ_0018818 knockdown suppresses tumorigenesis in non-small cell lung cancer by sponging miR-767-3p. [Abstract]

2020 May 1;12(9):7774-7785. PMID: 32357143
J Virol

PPP2R5B regulates ANPEP expression and TGEV entry via dephosphorylation of HSF1 at Ser304/Ser308. [Abstract]

2026 Jun 11:e0016626. PMID: 42274214
Stem Cells

DAPK1 Interacts with the p38 Isoform MAPK14, Preventing Its Nuclear Translocation and Stimulation of Bone Marrow Adipogenesis. [Abstract]

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Front Oncol

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Am J Cancer Res

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2020 Jan 1;10(1):224-236. PMID: 32064163
Virus Res

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Gene

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2022 Mar 30:816:146171. PMID: 35026293
Steroids

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Biochem Biophys Res Commun

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2020 Feb 15;12(2):478-492. PMID: 32194897
Curr Sci

2025 Oct 5.
Res Sq

2026 Apr 16.
bioRxiv

2026 Apr 9.
medRxiv

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bioRxiv

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State University of New York at Stony Brook

2025.
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bioRxiv

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bioRxiv

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bioRxiv

Pol II degradation activates cell death independently from the loss of transcription. [Abstract]

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bioRxiv

2024 September 07.
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Research Square Print

December 21st, 2022.
Research Square Preprint

2021 Oct.
Research Square Preprint

2020 Oct.
Radboud University Nijmegen

2019 Oct.
Oncotarget

Dual inhibition of AKT/FLT3-ITD by A674563 overcomes FLT3 ligand-induced drug resistance in FLT3-ITD positive AML. [Abstract]

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Solvant et solubilité

In Vitro:

DMSO : 125 mg/mL (291.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3314 mL

11.6572 mL

23.3144 mL

5 mM

0.4663 mL

2.3314 mL

4.6629 mL

10 mM

0.2331 mL

1.1657 mL

2.3314 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (4.85 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (4.85 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.85 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 10 mg/mL (23.31 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

Cell Assay^[1]

Cell proliferation assay is determined by 2 methods, MTS and Sytox Green. Briefly, cells are seeded in 96-well plates (at a density to allow for logarithmic growth during the 72-hour assay) and incubated overnight at 37°C, 5% CO₂. Cells are then exposed to concentrations of Capivasertib ranging from 30 to 0.003 μM for 72 hours. For the MTS endpoint, cell proliferation is measured by the CellTiter AQueous Non-Radioactive Cell Proliferation Assay reagent. Absorbance is measured with a Tecan Ultra instrument. 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 (GI₅₀) values are determined using absorbance readings (MTS) or live cell counts^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Mice^[1]
Specific, pathogen-free, female nude mice (nu/nu: Alpk) and male SCID mice (SCID/CB17; 786-0 xenograft studies) are used. When mean tumor sizes reach approximately 0.2 cm3, the mice are randomized into control and treatment groups. The treatment groups received varying dose schedules of Capivasertib (AZD5363) solubilized in a 10% DMSO 25% w/v Kleptose HPB (Roquette) buffer by oral gavage, RP-56976 solubilized in 2.6% ethanol in injectable water by intravenous injection once on day 1 at 15 or 5 mg/kg once weekly. When administered in combination, RP-56976 is administered 1 hour before the oral dose of Capivasertib (AZD5363). The control group received the DMSO/Kleptose buffer alone, twice daily by oral gavage. Tumor volumes (measured by caliper), animal body weight, and tumor condition are recorded twice weekly for the duration of the study. Mice are sacrificed by CO2 euthanasia. The tumor volume is calculated (taking length to be the longest diameter across the tumor and width to be the corresponding perpendicular diameter) using the formula: (length×width)×√(length×width)×(π/6). Growth inhibition from the start of treatment is assessed by comparison of the differences in tumor volume between control and treated groups.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (284 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Davies BR, et al. Preclinical pharmacology of AZD5363, an inhibitor of AKT: pharmacodynamics, antitumor activity, and correlation of monotherapy activity with genetic background. Mol Cancer Ther. 2012 Apr;11(4):873-87. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3314 mL	11.6572 mL	23.3144 mL	58.2859 mL
	5 mM	0.4663 mL	2.3314 mL	4.6629 mL	11.6572 mL
	10 mM	0.2331 mL	1.1657 mL	2.3314 mL	5.8286 mL
	15 mM	0.1554 mL	0.7771 mL	1.5543 mL	3.8857 mL
	20 mM	0.1166 mL	0.5829 mL	1.1657 mL	2.9143 mL
	25 mM	0.0933 mL	0.4663 mL	0.9326 mL	2.3314 mL
	30 mM	0.0777 mL	0.3886 mL	0.7771 mL	1.9429 mL
	40 mM	0.0583 mL	0.2914 mL	0.5829 mL	1.4571 mL
	50 mM	0.0466 mL	0.2331 mL	0.4663 mL	1.1657 mL
	60 mM	0.0389 mL	0.1943 mL	0.3886 mL	0.9714 mL
	80 mM	0.0291 mL	0.1457 mL	0.2914 mL	0.7286 mL
	100 mM	0.0233 mL	0.1166 mL	0.2331 mL	0.5829 mL

Keywords

Capivasertib

89 Cited Publications

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Capivasertib

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Publications Citing Use of MedChemExpress (MCE) Capivasertib

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Chemical Information

Publications (89)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Capivasertib Related Classifications

HY-15431 Related Classifications