Uprosertib (GSK2141795)

Catalog No.S7492 Synonyms: GSK795

Uprosertib (GSK2141795) Chemical Structure

Molecular Weight(MW): 429.25

Uprosertib (GSK2141795) is a selective, ATP-competitive, and orally bioavailable Akt inhibitor with IC50 of 180 nM, 328 nM, and 38 nM for Akt 1, 2 and 3, respectively. Phase 2.

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1 Customer Review

  • Parental cell line wastreated with Akt inhibitor (GSK2141795) and BGJ398. The 5 uM BGJ398 resistant cell line was treated with GSK2141795, BGJ398, and 2 concentrations of GSK2141795 and varying dosages of BGJ398. The parental cell line treated with GSK2141795, the dark green line, indicates minimal effect of the inhibitor compared to the resistant cell line treated GSK2141795, the light purple line. However, when the resistant cell line is treated with both GSK2141795 and BGJ398 there is a greater decrease in cell viability compared to the resistant cell line that is treated only with GSK2141795.

    The Ohio State University, 2015. Uprosertib (GSK2141795) purchased from Selleck.

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Biological Activity

Description Uprosertib (GSK2141795) is a selective, ATP-competitive, and orally bioavailable Akt inhibitor with IC50 of 180 nM, 328 nM, and 38 nM for Akt 1, 2 and 3, respectively. Phase 2.
Targets
Akt3 [1]
(Cell-free assay)
Akt1 [1]
(Cell-free assay)
Akt2 [1]
(Cell-free assay)
38 nM 180 nM 328 nM
In vitro

Uprosertib inhibits multiple AKT substrate phosphorylation levels, including GSK3β, PRAS40, FOXO and Caspase 9 in both BT474 and LNCaP cells. Uprosertib preferentially inhibits the proliferation of human cancer cells lines with AKT pathway activation. In LNCaP, BT474, A3 and I9.2 cells lines, Uprosertib also causes cell cycle arrest. [2] In both SKOV3 and PEO4 cells, Uprosertib causes growth-arrest as single agent, and enhances cisplatin-induced apoptosis. [3]

In vivo In mice bearing BT474 breast tumor xenografts, Uprosertib (100 mg/kg, p.o.) results 61% tumor growth inhibition. In mice bearing SKOV3 ovarian tumor xenografts, Uprosertib (30 mg/kg, p.o.) results 61% tumor growth inhibition. [2]

Protocol

Kinase Assay:[1]
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Selectivity profiling experiments:

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 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.
Cell Research:[2]
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  • Cell lines: A panel of 290 cells lines
  • Concentrations: ~30 μM
  • Incubation Time: 3 d
  • Method: Cell lines are typically grown in RPMI 160 medium containing 10% FBS. Some cell lines are grown in media specified by the vendor. A 3-day proliferation assay using CellTiter-Glo is performed to measure the growth inhibition by the compounds at 0–30 µM. Cell growth is determined relative to untreated (DMSO) controls. EC50's are calculated from inhibition curves using a 4- or 6-parameter fitting algorithm in the Assay Client application.
    (Only for Reference)
Animal Research:[2]
+ Expand
  • Animal Models: Mice bearing either BT474 or SKOV3 tumors
  • Formulation: 20% polyethylene glycol (PEG) 400/1% DMSO
  • Dosages: 100 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 85 mg/mL (198.01 mM)
Ethanol 85 mg/mL (198.01 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 429.25
Formula

C18H16Cl2F2N4O2

CAS No. 1047634-65-0
Storage powder
Synonyms GSK795

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Clinical Trial Information

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
NCT01907815 Active, not recruiting Recurrent Adult Acute Myeloid Leukemia|Untreated Adult Acute Myeloid Leukemia National Cancer Institute (NCI) October 2013 Phase 2
NCT01989598 Active, not recruiting Recurrent Plasma Cell Myeloma|Refractory Plasma Cell Myeloma National Cancer Institute (NCI) October 2013 Phase 2
NCT01964924 Recruiting Estrogen Receptor Negative|HER2/Neu Negative|Invasive Breast Carcinoma|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Stage IV Breast Cancer|Triple-Negative Breast Carcinoma National Cancer Institute (NCI)|GlaxoSmithKline October 2013 Phase 2
NCT01979523 Recruiting Recurrent Uveal Melanoma|Stage IV Uveal Melanoma National Cancer Institute (NCI) October 2013 Phase 2
NCT01941927 Unknown status Melanoma Adil Daud|National Comprehensive Cancer Network|University of California, San Francisco September 2013 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID