Uprosertib
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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.93%
- CAS No.: 1047634-65-0
- Formule: C18H16Cl2F2N4O2
- Masse moléculaire:429.25
-
Stockage:
-20°C, stored under nitrogen
* In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
-
Solvant et solubilité
- Pureté et documentation
- Références
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Uprosertib
More- Immunity. 2020 Jan 14;52(1):109-122.e6. [Abstract]
- Nat Commun. 2022 Nov 29;13(1):7345. [Abstract]
- Nat Commun. 2017 Sep 4;8(1):410. [Abstract]
- Cancer Biol Med. 2021 Mar 12;19(1):104-119. [Abstract]
- Clin Cancer Res. 2016 Nov 15;22(22):5514-5526. [Abstract]
- NPJ Precis Oncol. 2021 Jul 15;5(1):65. [Abstract]
- Cell Prolif. 2026 Apr 22:e70214. [Abstract]
- Mol Cancer Ther. 2017 Apr;16(4):614-624. [Abstract]
- Ecotoxicol Environ Saf. 2021 Sep 15:221:112447. [Abstract]
- Oncoimmunology. 2018 Aug 6;7(10):e1488565. [Abstract]
- Biol Proced Online. 2025 Oct 15;27(1):39. [Abstract]
- iScience. 2023 Jun 7;26(7):107025. [Abstract]
- J Biol Chem. 2024 Feb;300(2):105641. [Abstract]
- Cell Biol Int. 2020 Feb;44(2):610-620. [Abstract]
- Biomed Res Int. 2019 May 16:2019:2821731. [Abstract]
- Meat and Muscle Biology. 2026.
- Research Square Preprint. 2021 Sep.
- Radboud University Nijmegen. 2019 Oct.
- Oncotarget. 2018 Jul 31;9(59):31549-31558. [Abstract]
- Methods Mol Biol. 2018:1711:351-398. [Abstract]
Customer Validation & Images
-
WB
-
WB
-
WB
Activité biologique
|
Akt3 38 nM (IC50) |
Akt1 180 nM (IC50) |
Akt2 328 nM (IC50) |
ROCK1 1570 nM (IC50) |
ROCK2 1850 nM (IC50) |
CDK7 2100 nM (IC50) |
|
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] |
Uprosertib (GSK2141795) inhibits Akt1/2/3 with the Kd 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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 1047634-65-0
-
Appearance Solid
-
Masse moléculaire 429.25
-
Formule 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
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
-20°C, stored under nitrogen
* In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)
Publications (20)
-
Journal Impact Factor
-
Most Recent
-
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
2022 Nov 29;13(1):7345. PMID: 36446858 -
Nat Commun
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 -
-
-
-
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
2018:1711:351-398. PMID: 29344898
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
Please enter the basic information of animal 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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
-
Fiche technique (275 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)
-
Instruction de manipulation (2659 KB)
Références
[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]
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 (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.
| 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 |
Uprosertib Related Classifications
HY-15965 Related Classifications
Powered by Bioz