Name: Uprosertib (GSK2141795)
Brand: Selleck Chemicals
SKU: S7492
Availability: InStock
Rating: 5 (13 reviews)

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Quality Control

Batch: Purity: 99.84%

99.84

Related Targets	PI3K mTOR GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A PDK
Other Akt Inhibitors	SC79 Ipatasertib (GDC-0068) MK-2206 Dihydrochloride Perifosine AZD5363 (Capivasertib) GSK690693 Triciribine (API-2) CCT128930 Afuresertib (GSK2110183) A-674563 HCl

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
OVCAR8	Antiproliferative assay		Antiproliferative activity against human OVCAR8 cells, IC50=0.24μM	31298542
Sf9	Function assay	40 mins	Inhibition of full length human AKT1 expressed in Sf9 cells assessed as reduction in substrate phosphorylation using biotin-ahx-ARKRERAYSFGHHA-amide substrate and [gamma-33P]ATP incubated for 40 mins by top count microplate scintillation counting method, IC50=0.001995μM	ChEMBL
JVM2	Antiproliferative assay		Antiproliferative activity against human JVM2 cells assessed as reduction in cell viability, IC50=0.293μM	31301565
KB-3-1	qHTS assay		P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	ChEMBL
HUT78	Antiproliferative assay		Antiproliferative activity against human HUT78 cells assessed as reduction in cell viability, IC50=0.378μM	31301565
Sf9	Function assay	40 mins	Inhibition of full length human AKT2 expressed in Sf9 cells assessed as reduction in substrate phosphorylation using biotin-ahx-ARKRERAYSFGHHA-amide substrate and [gamma-33P]ATP incubated for 40 mins by top count microplate scintillation counting method, IC50=0.01585μM	ChEMBL
CEM/C1	Antiproliferative assay		Antiproliferative activity against human CEM/C1 cells assessed as reduction in cell viability, IC50=0.03μM	31301565
RPMI8226	Antiproliferative assay		Antiproliferative activity against human RPMI8226 cells assessed as reduction in cell viability, IC50=0.538μM	31301565
MM1S	Antiproliferative assay		Antiproliferative activity against human MM1S cells assessed as reduction in cell viability, IC50=0.032μM	31301565
OVCAR8	Cytotoxicity assay	72 hrs	Cytotoxicity against human OVCAR8 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay, IC50=0.54μM	31301565
MOLT4	Antiproliferative assay		Antiproliferative activity against human MOLT4 cells assessed as reduction in cell viability, IC50=0.066μM	31301565
MV4-11	Antiproliferative assay		Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability, IC50=0.635μM	31301565
LNCAP	Antiproliferative assay		Antiproliferative activity against human LNCAP cells, IC50=0.07μM	31298542
HCT116	Antiproliferative assay	72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay, IC50=0.72μM	31298542
PTEN-null LNCAP	Function assay	1 hr	Inhibition of Akt in human PTEN-null LNCAP cells assessed as suppression in PRAS40 phosphorylation after 1 hr by ELISA analysis, IC50=0.07563μM	27089211
HCT116	Growth inhibition assay	72 hrs	Growth inhibition of human HCT116 cells over-expressing DHODH at 2 times antiproliferative IC50 after 72 hrs in absence of uridine by MTT assay	31301565
U937	Antiproliferative assay		Antiproliferative activity against human U937 cells assessed as reduction in cell viability, IC50=0.101μM	31301565
OVCAR8	Antiproliferative assay		Antiproliferative activity against human OVCAR8 cells, IC50=0.24μM	31298542
JVM2	Antiproliferative assay		Antiproliferative activity against human JVM2 cells assessed as reduction in cell viability, IC50=0.293μM	31301565
HUT78	Antiproliferative assay		Antiproliferative activity against human HUT78 cells assessed as reduction in cell viability, IC50=0.378μM	31301565
RPMI8226	Antiproliferative assay		Antiproliferative activity against human RPMI8226 cells assessed as reduction in cell viability, IC50=0.538μM	31301565
OVCAR8	Cytotoxicity assay	72 hrs	Cytotoxicity against human OVCAR8 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay, IC50=0.54μM	31301565
MV4-11	Antiproliferative assay		Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability, IC50=0.635μM	31301565
HCT116	Antiproliferative assay	72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay, IC50=0.72μM	31298542
HCT116	Growth inhibition assay	72 hrs	Growth inhibition of human HCT116 cells over-expressing DHODH at 2 times antiproliferative IC50 after 72 hrs in absence of uridine by MTT assay	31301565
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 85 mg/mL (198.01 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 85 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.250mg/ml (9.90mM)	Taking the 1 mL working solution as an example, add 50 μL of 85 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.710mg/ml (1.65mM)	Taking the 1 mL working solution as an example, add 50 μL of 14.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	429.25	Formula	C₁₈H₁₆C_l2F₂N₄O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1047634-65-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	GSK795			Smiles	CN1C(=C(C=N1)Cl)C2=C(OC(=C2)C(=O)NC(CC3=CC(=C(C=C3)F)F)CN)Cl

Mechanism of Action

Targets/IC₅₀/Ki	Akt3 (Cell-free assay) 38 nM Akt1 (Cell-free assay) 180 nM Akt2 (Cell-free assay) 328 nM
In vitro	Uprosertib (GSK2141795) inhibits multiple AKT substrate phosphorylation levels, including GSK3β, PRAS40, FOXO and Caspase 9 in both BT474 and LNCaP cells. It preferentially inhibits the proliferation of human cancer cells lines with AKT pathway activation. In LNCaP, BT474, A3 and I9.2 cells lines, this compound also causes cell cycle arrest. In both SKOV3 and PEO4 cells, it causes growth-arrest as single agent, and enhances induced apoptosis.
Kinase Assay	Selectivity profiling experiments
Kinase Assay	The lysates (5 mg of total protein each) are preincubated with 0 (DMSO control), 2.5 nM, 25 nM, 250 nM, 2.5 μM or 25 μM free compound (GSK690693 or Uprosertib (GSK2141795)) on an end-over-end shaker for 45 min at 4 °C. Subsequently, lysates are incubated with beads (coupled Akt probe or kinobeads) for 1 h at 4 °C, for both qualitative and quantitative experiments. The beads are washed with 1× CP buffer and collected by centrifugation. Bound proteins are eluted with 2× NuPAGE LDS sample buffer, and eluates are reduced and alkylated by 50 mM dithiothreitol and 55 mM iodoacetamide.
In vivo	In mice bearing BT474 breast tumor xenografts, Uprosertib (GSK2141795) (100 mg/kg, p.o.) results in 61% tumor growth inhibition. This compound also produces 61% tumor growth inhibition in mice bearing SKOV3 ovarian tumor xenografts at a dose of 30 mg/kg, p.o.
References	[1] https://pubmed.ncbi.nlm.nih.gov/23795919/ [2] https://pubmed.ncbi.nlm.nih.gov/24978597/ [3] https://pubmed.ncbi.nlm.nih.gov/26497682/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01958112	Terminated	Cervical Cancer	Dana-Farber Cancer Institute\|Novartis\|National Comprehensive Cancer Network	October 2013	Phase 2
NCT01941927	Completed	Melanoma	Adil Daud\|National Comprehensive Cancer Network\|University of California San Francisco	September 10 2013	Phase 2
NCT01266954	Completed	Solid Tumours	GlaxoSmithKline	June 1 2010	Phase 1
NCT01138085	Completed	Cancer	GlaxoSmithKline	May 4 2010	Phase 1

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Uprosertib (GSK2141795) Akt inhibitor

Chemical Structure

Molecular Weight: 429.25