Afuresertib hydrochloride (Synonyms: GSK2110183 hydrochloride; LAE002 hydrochloride)

Name: Afuresertib hydrochloride
Brand: MedChemExpress
SKU: HY-15727A
Rating: 5.0 (16 reviews)

Cat. No.: HY-15727A Purity: 99.95%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Afuresertib hydrochloride (GSK 2110183 hydrochloride) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with K_is of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively.

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

Afuresertib hydrochloride Chemical Structure

CAS No. : 1047645-82-8

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 92	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 92	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 84	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 114	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 324	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 564	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 16 publication(s) in Google Scholar

Other Forms of Afuresertib hydrochloride:

Afuresertib In-stock

15 Publications Citing Use of MCE Afuresertib hydrochloride

Proliferation Assay

: Afuresertib hydrochloride purchased from MedChemExpress. Usage Cited in: J Physiol. 2017 Jul 1;595(13):4207-4225. [Abstract]; Effects of pharmacological inhibitors on AngII-mediated activation of L-type Ca²⁺ channels in NVCMs. NVCMs are treated with vehicle, Erlotinib, H-89, Afuresertib (1 μM), Gö6983, CID755673, KN-93, SCH772984, Bosutinib or Quinalizarin for 30 min before treatment of AngII.

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Akt Akt1 Akt2 Akt3

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PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

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ROCK ROCK1 ROCK2

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[2]

Akt1

0.08 nM (Ki)

Akt2

2 nM (Ki)

Akt3

2.6 nM (Ki)

Akt1 E17K mutant

0.2 nM (IC₅₀)

PKCη

210 nM (IC₅₀)

PKC-βI

430 nM (IC₅₀)

ROCK

100 nM (IC₅₀)

PKCθ

510 nM (IC₅₀)

In Vitro

Afuresertib (GSK 2110183) exhibits favorable tumor-suppressive effects on malignant pleural mesothelioma (MPM) cells. Afuresertib significantly increases caspase-3 and caspase-7 activities and apoptotic cell number among ACC-MESO-4 and MSTO-211H cells. Afuresertib strongly arrests the cell cycle in the G₁ phase.
Western blotting analysis shows that Afuresertib increases the expression of p21^WAF1/CIP1 and decreases the phosphorylation of Akt substrates, including GSK-3β and FOXO family proteins. Afuresertib-induced p21 expression promotes G₁ phase arrest by inducing FOXO activity. Afuresertib significantly enhances cisplatin-induced cytotoxicity. Afuresertib modulates the expression E2F1 and MYC, which are associated with fibroblast core serum response^[1].

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

In Vivo

Mice bearing BT474 breast tumor xenografts are dosed orally with either vehicle or GSK2110183 at 10, 30 or 100 mg/kg daily for 21 days which result in 8, 37 and 61% TGI, respectively. Mice tolerated GSK2110183 well, with 1-3% body weight loss reported after 5 days of dosing which recover over the course of the study. Other tumor xenograft models which possess an activation of the Akt pathway are explored to further demonstrate compound efficacy. Mice treated with GSK2110183 at 10, 30 and 100 mg/kg result in 23, 37 and 97% TGI, respectively, of SKOV3 xenografts^[2].

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

Clinical Trial

Molecular Weight

463.78

Formula

C₁₈H₁₈Cl₃FN₄OS

CAS No.

1047645-82-8

Appearance

Solid

Color

White to yellow

SMILES

O=C(C1=CC(C2=C(Cl)C=NN2C)=C(Cl)S1)N[C@@H](CC3=CC=CC(F)=C3)CN.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (215.62 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	2.1562 mL	10.7810 mL	21.5619 mL
5 mM	0.4312 mL	2.1562 mL	4.3124 mL
10 mM	0.2156 mL	1.0781 mL	2.1562 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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
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)

Volume _(start)

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: ≥ 2.5 mg/mL (5.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

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 (280 KB) SDS (393 KB)

COA (254 KB) HNMR (281 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Yamaji M, et al. Novel ATP-competitive Akt inhibitor Afuresertib suppresses the proliferation of malignant pleural mesothelioma cells. Cancer Med. 2017 Nov;6(11):2646-2659. [Content Brief]

[2]. Dumble M, et al. Discovery of novel AKT inhibitors with enhanced anti-tumor effects in combination with the MEK inhibitor. PLoS One. 2014 Jun 30;9(6):e100880 [Content Brief]

Cell Assay
^[1]

MPM cells are seeded in 96-well plates (cell density, 2.5×10³ cells/well) and are incubated for 24 h at 37°C. Next, the cells are incubated in a medium containing indicated concentrations of Akt inhibitors (e.g., Afuresertib ; 50, 20, 10, 5, 2, 1, 0.5, 0.2, 0.1, and 0.01 μM) for 72 h. Next, MTT solution is added to each well, and the cells are incubated for 4 h. Finally, the cells are incubated overnight with lysis buffer (10% SDS in 0.01 mol/L hydrogen chloride). Absorbance is measured at 550 nm using SpectraMAX M5 spectrophotometer^[1].

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

References

[1]. Yamaji M, et al. Novel ATP-competitive Akt inhibitor Afuresertib suppresses the proliferation of malignant pleural mesothelioma cells. Cancer Med. 2017 Nov;6(11):2646-2659. [Content Brief]

[2]. Dumble M, et al. Discovery of novel AKT inhibitors with enhanced anti-tumor effects in combination with the MEK inhibitor. PLoS One. 2014 Jun 30;9(6):e100880 [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1562 mL	10.7810 mL	21.5619 mL	53.9049 mL
	5 mM	0.4312 mL	2.1562 mL	4.3124 mL	10.7810 mL
	10 mM	0.2156 mL	1.0781 mL	2.1562 mL	5.3905 mL
	15 mM	0.1437 mL	0.7187 mL	1.4375 mL	3.5937 mL
	20 mM	0.1078 mL	0.5390 mL	1.0781 mL	2.6952 mL
	25 mM	0.0862 mL	0.4312 mL	0.8625 mL	2.1562 mL
	30 mM	0.0719 mL	0.3594 mL	0.7187 mL	1.7968 mL
	40 mM	0.0539 mL	0.2695 mL	0.5390 mL	1.3476 mL
	50 mM	0.0431 mL	0.2156 mL	0.4312 mL	1.0781 mL
	60 mM	0.0359 mL	0.1797 mL	0.3594 mL	0.8984 mL
	80 mM	0.0270 mL	0.1348 mL	0.2695 mL	0.6738 mL
	100 mM	0.0216 mL	0.1078 mL	0.2156 mL	0.5390 mL

Afuresertib hydrochloride 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.

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Afuresertib hydrochloride (Synonyms: GSK2110183 hydrochloride; LAE002 hydrochloride)

Customer Review

Other Forms of Afuresertib hydrochloride:

Afuresertib hydrochloride Related Antibodies

15 Publications Citing Use of MCE Afuresertib hydrochloride

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Akt Isoform Specific Products:

View All PKC Isoform Specific Products:

View All ROCK Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Afuresertib hydrochloride Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Afuresertib hydrochloride Related Classifications

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Customer Review

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