Art. -Nr.: HY-15965

Uprosertib

Name: Uprosertib
Brand: MedChemExpress
SKU: HY-15965
Price: 99.00 USD
Availability: InStock
Rating: 5 (20 reviews)

(Synonyms: GSK2141795)

20 Cited Publications

Kundenbewertung

Based on 20 publication(s) in Google Scholar

Uprosertib (GSK2141795) is a potent and selective pan-Akt inhibitor with IC₅₀ values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.

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Reinheit: 99.93%
CAS. Nr.: 1047634-65-0
Formel: C₁₈H₁₆Cl₂F₂N₄O₂
Molecular Weight:429.25

Speicherung:

-20°C, stored under nitrogen

* In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)

Uprosertib Chemical Structure

CAS. Nr.: 1047634-65-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Clinical Trial
Chemical Information
Publications (20)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Uprosertib (GSK2141795) is a potent and selective pan-Akt inhibitor with IC₅₀ values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.

IC₅₀ & Target

^[1]

Akt3

38 nM (IC₅₀)

Akt1

180 nM (IC₅₀)

Akt2

328 nM (IC₅₀)

ROCK1

1570 nM (IC₅₀)

ROCK2

1850 nM (IC₅₀)

CDK7

2100 nM (IC₅₀)

Alle Akt Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	0.72 μM Compound: GSK2141795; GSK-795	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	1.75 μM Compound: GSK2141795	Cytotoxicity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Cytotoxicity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 31301565]
HuT78	IC₅₀	378 nM Compound: GSK2141795	Antiproliferative activity against human HUT78 cells assessed as reduction in cell viability Antiproliferative activity against human HUT78 cells assessed as reduction in cell viability	[PMID: 31301565]
JVM-2	IC₅₀	293 nM Compound: GSK2141795	Antiproliferative activity against human JVM2 cells assessed as reduction in cell viability Antiproliferative activity against human JVM2 cells assessed as reduction in cell viability	[PMID: 31301565]
K562	IC₅₀	>3000 nM Compound: GSK2141795	Antiproliferative activity against human K562 cells assessed as reduction in cell viability Antiproliferative activity against human K562 cells assessed as reduction in cell viability	[PMID: 31301565]
LNCaP	IC₅₀	75.63 nM Compound: GSK2141795	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	0.07 μM Compound: GSK2141795; GSK-795	Antiproliferative activity against human LNCAP cells Antiproliferative activity against human LNCAP cells	[PMID: 31298542]
MM1.S	IC₅₀	32 nM Compound: GSK2141795	Antiproliferative activity against human MM1S cells assessed as reduction in cell viability Antiproliferative activity against human MM1S cells assessed as reduction in cell viability	[PMID: 31301565]
MOLT-4	IC₅₀	66 nM Compound: GSK2141795	Antiproliferative activity against human MOLT4 cells assessed as reduction in cell viability Antiproliferative activity against human MOLT4 cells assessed as reduction in cell viability	[PMID: 31301565]
MV4-11	IC₅₀	635 nM Compound: GSK2141795	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability	[PMID: 31301565]
OVCAR-8	IC₅₀	0.24 μM Compound: GSK2141795; GSK-795	Antiproliferative activity against human OVCAR8 cells Antiproliferative activity against human OVCAR8 cells	[PMID: 31298542]
OVCAR-8	IC₅₀	0.54 μM Compound: GSK2141795	Cytotoxicity against human OVCAR8 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Cytotoxicity against human OVCAR8 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 31301565]
RPMI-8226	IC₅₀	538 nM Compound: GSK2141795	Antiproliferative activity against human RPMI8226 cells assessed as reduction in cell viability Antiproliferative activity against human RPMI8226 cells assessed as reduction in cell viability	[PMID: 31301565]
U-937	IC₅₀	101 nM Compound: GSK2141795	Antiproliferative activity against human U937 cells assessed as reduction in cell viability Antiproliferative activity against human U937 cells assessed as reduction in cell viability	[PMID: 31301565]

In Vitro

Uprosertib (GSK2141795) inhibits Akt1/2/3 with the K_d values of 16/49/5 nM, respectively. Uprosertib potently inhibits only the PKC family members PRKACA and PRKACB as well as the cGMP-dependent protein kinase PRKG1 aqpart from the Akts. Protein targets that bind Uprosertib (GSK2141795) in the lysate show a dose-dependent reduction in binding to the kinobeads, while proteins unaffected by the drug show no reduction in binding^[1].

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

Clinical Trial

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

Chemical Information

CAS. Nr. 1047634-65-0
Appearance Solid
Molecular Weight 429.25
Formel C₁₈H₁₆Cl₂F₂N₄O₂
Color White to off-white
SMILES

O=C(C1=CC(C2=C(Cl)C=NN2C)=C(Cl)O1)N[C@@H](CC3=CC=C(F)C(F)=C3)CN
Synonyms

GSK2141795
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, stored under nitrogen

* In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)

Publications (20)

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Journal Impact Factor

Immunity

Targeting 7-Dehydrocholesterol Reductase Integrates Cholesterol Metabolism and IRF3 Activation to Eliminate Infection. [Abstract]

2020 Jan 14;52(1):109-122.e6. PMID: 31882361
Nat Commun

IL6 supports long-term expansion of hepatocytes in vitro. [Abstract]

2022 Nov 29;13(1):7345. PMID: 36446858
Nat Commun

Convergent Akt activation drives acquired EGFR inhibitor resistance in lung cancer. [Abstract]

2017 Sep 4;8(1):410. PMID: 28871105

Uprosertib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2017 Sep 4;8(1):410. [Abstract]

Effect of EGFR TKIs and Akt inhibitors on key signal transduction proteins in parental and resistant PC9 cells. Western blot analysis of PC9 and PC9-ER treated for 4 h with Erlotinib (30 µM), GSK2141795 (2.5 µM) or the combination.
Cancer Biol Med

SNORA23 inhibits HCC tumorigenesis by impairing the 2'-O-ribose methylation level of 28S rRNA. [Abstract]

2021 Mar 12;19(1):104-119. PMID: 33710804
Clin Cancer Res

High CDK6 Protects Cells from Fulvestrant-Mediated Apoptosis and is a Predictor of Resistance to Fulvestrant in Estrogen Receptor-Positive Metastatic Breast Cancer. [Abstract]

2016 Nov 15;22(22):5514-5526. PMID: 27252418
NPJ Precis Oncol

Combined FGFR and Akt pathway inhibition abrogates growth of FGFR1 overexpressing EGFR-TKI-resistant NSCLC cells. [Abstract]

2021 Jul 15;5(1):65. PMID: 34267282
Cell Prolif

Targeting Egfr-Mediated Cell Proliferation and Lipid Metabolism Separation Effectively Accelerate Liver Regeneration. [Abstract]

2026 Apr 22:e70214. PMID: 42019507
Mol Cancer Ther

Akt Activation Mediates Acquired Resistance to Fibroblast Growth Factor Receptor Inhibitor BGJ398. [Abstract]

2017 Apr;16(4):614-624. PMID: 28255027

Uprosertib purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2017 Apr;16(4):614-624. [Abstract]

Western blot analysis is performed with lysates from resistant cell lines treated either with vehicle (DMSO) or GSK2141795 (1 μM) for 24 hours to assess inhibition of Akt (pAKT) and downstream (pGSK3) signaling (three experimental replicates).
Ecotoxicol Environ Saf

Clusterin inhibits Cr(VI)-induced apoptosis via enhancing mitochondrial biogenesis through AKT-associated STAT3 activation in L02 hepatocytes. [Abstract]

2021 Sep 15:221:112447. PMID: 34175824
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
Biol Proced Online

Rap2B-mediated reprogramming of the PI3K/AKT signaling axis drives resistance to cetuximab-targeted therapy in colorectal carcinoma. [Abstract]

2025 Oct 15;27(1):39. PMID: 41094393
iScience

Resistin targets TAZ to promote osteogenic differentiation through PI3K/AKT/mTOR pathway. [Abstract]

2023 Jun 7;26(7):107025. PMID: 37389179
J Biol Chem

Disruption of lysosomal nutrient sensing scaffold contributes to pathogenesis of a fatal neurodegenerative lysosomal storage disease. [Abstract]

2024 Feb;300(2):105641. PMID: 38211816
Cell Biol Int

Reversing microtubule-directed chemotherapeutic drug resistance by co-delivering α2β1 inhibitor and paclitaxel with nanoparticles in ovarian cancer. [Abstract]

2020 Feb;44(2):610-620. PMID: 31743535
Biomed Res Int

MiR-21-3p Plays a Crucial Role in Metabolism Alteration of Renal Tubular Epithelial Cells during Sepsis Associated Acute Kidney Injury via AKT/CDK2-FOXO1 Pathway. [Abstract]

2019 May 16:2019:2821731. PMID: 31223614
Meat and Muscle Biology

2026.
Research Square Preprint

2021 Sep.
Radboud University Nijmegen

2019 Oct.
Oncotarget

Deep analysis of acquired resistance to FGFR1 inhibitor identifies MET and AKT activation and an expansion of AKT1 mutant cells. [Abstract]

2018 Jul 31;9(59):31549-31558. PMID: 30140389

Uprosertib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2018 Jul 31;9(59):31549-31558. [Abstract]

Western blots of the indicated proteins in the DMS114-P and DMS114-R cells treated with (+) and without (-) the AKT inhibitor, Uprosertib (200 nM) for 6 h (left panel) or 24 h (right panel). In the case of DMS114-P, extracts with (+) and without (-) treatment with PD173074 (1 µM) are also shown.
Methods Mol Biol

Methods for High-throughput Drug Combination Screening and Synergy Scoring. [Abstract]

2018:1711:351-398. PMID: 29344898

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (116.48 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

2.3296 mL

11.6482 mL

23.2964 mL

5 mM

0.4659 mL

2.3296 mL

4.6593 mL

10 mM

0.2330 mL

1.1648 mL

2.3296 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 (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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: ≥ 2.5 mg/mL (5.82 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.

Protocol 2

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

Solubility: 2.5 mg/mL (5.82 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

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.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (5.82 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 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (643 KB)
- English - EN (643 KB)
- Français - FR (643 KB)
- Deutsch - DE (643 KB)
- Norwegian - NO (643 KB)
- Español - ES (643 KB)
- Swedish - SV (643 KB)
- Italian - IT (643 KB)
- Korean - KR (643 KB)
- Portuguese - PT (643 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)
Handling Instructions (2659 KB)

Verweise

[1]. Pachl F, et al. Characterization of a chemical affinity probe targeting Akt kinases. J Proteome Res. 2013 Aug 2;12(8):3792-800. [Content Brief]

[2]. Jacobsen K, et al. Convergent Akt activation drives acquired EGFR inhibitor resistance in lung cancer. Nat Commun. 2017 Sep 4;8(1):410. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3296 mL	11.6482 mL	23.2964 mL	58.2411 mL
	5 mM	0.4659 mL	2.3296 mL	4.6593 mL	11.6482 mL
	10 mM	0.2330 mL	1.1648 mL	2.3296 mL	5.8241 mL
	15 mM	0.1553 mL	0.7765 mL	1.5531 mL	3.8827 mL
	20 mM	0.1165 mL	0.5824 mL	1.1648 mL	2.9121 mL
	25 mM	0.0932 mL	0.4659 mL	0.9319 mL	2.3296 mL
	30 mM	0.0777 mL	0.3883 mL	0.7765 mL	1.9414 mL
	40 mM	0.0582 mL	0.2912 mL	0.5824 mL	1.4560 mL
	50 mM	0.0466 mL	0.2330 mL	0.4659 mL	1.1648 mL
	60 mM	0.0388 mL	0.1941 mL	0.3883 mL	0.9707 mL
	80 mM	0.0291 mL	0.1456 mL	0.2912 mL	0.7280 mL
	100 mM	0.0233 mL	0.1165 mL	0.2330 mL	0.5824 mL

Bioz

Keywords

Uprosertib

20 Cited Publications

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Uprosertib

Publications Citing Use of MedChemExpress (MCE) Uprosertib

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