Capivasertib (Synonyms: AZD5363)

Name: Capivasertib
Brand: MedChemExpress
SKU: HY-15431
Rating: 5.0 (57 reviews)

Cat. No.: HY-15431 Purity: 99.95%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

Capivasertib Chemical Structure

CAS No. : 1143532-39-1

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 106	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 106	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 96	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 144	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 260	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 360	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 480	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 1450	In-stock	Estimated Time of Arrival: December 31
1 g	USD 2200	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 57 publication(s) in Google Scholar

Other Forms of Capivasertib:

(R)-Capivasertib Get quote

56 Publications Citing Use of MCE Capivasertib

: Capivasertib purchased from MedChemExpress. Usage Cited in: Autophagy. 2021 Jun;17(6):1349-1366. [Abstract]; MiaPaca2 cells are treated with 25 μM AZD5363 (AKT inhibitor), 0.1 μM AZD2014 (MTOR inhibitor) for 24 h. Expression of RPS6, p-RPS6, lipidated and non-lipidated MAP1LC3B and ACTB proteins are determined by immunoblotting.

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Akt Akt1 Akt2 Akt3

Biological Activity
Protocol
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References
Customer Review

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

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]
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]
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: 31298542]
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]
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]
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]
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]
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-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]
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]
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]
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]
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	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]
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]
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]
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]
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]
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]

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.

Clinical Trial

Molecular Weight

428.92

Formula

C₂₁H₂₅ClN₆O₂

CAS No.

1143532-39-1

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

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Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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

Please enter your animal formula composition:

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Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.95%

Select Batch:

Data Sheet (284 KB) SDS (393 KB)

COA (256 KB) HNMR (300 KB) LCMS (97 KB)

Handling Instructions (2659 KB)

References

[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]

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]. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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]

Complete Stock Solution Preparation Table

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

Capivasertib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Capivasertib1143532-39-1AZD5363AZD 5363AZD-5363AktAutophagyPKBProtein kinase BInhibitorinhibitorinhibit

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Capivasertib (Synonyms: AZD5363)

Customer Review

Other Forms of Capivasertib:

Capivasertib Related Antibodies

56 Publications Citing Use of MCE Capivasertib

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Akt Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Capivasertib Related Antibodies

Molarity Calculator

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Complete Stock Solution Preparation Table

Capivasertib Related Classifications

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