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Uprosertib

Catalog No. T6849   CAS 1047634-65-0
Synonyms: GSK2141795, GSK795

Uprosertib (GSK2141795) (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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Uprosertib Chemical Structure
Uprosertib, CAS 1047634-65-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 39.00
2 mg In stock $ 54.00
5 mg In stock $ 77.00
10 mg In stock $ 126.00
25 mg In stock $ 212.00
50 mg In stock $ 340.00
100 mg In stock $ 563.00
200 mg In stock $ 791.00
1 mL * 10 mM (in DMSO) In stock $ 110.00
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Purity: 99.54%
Purity: 99.33%
Purity: 95.62%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Uprosertib (GSK2141795) (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&IC50 Akt1:180 nM, Akt2:328 nM, Akt3:38 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]
Kinase Assay 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 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)
Synonyms GSK2141795, GSK795
Molecular Weight 429.25
Formula C18H16Cl2F2N4O2
CAS No. 1047634-65-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 76 mg/mL(177.1 mM)

DMSO: 79 mg/mL (184 mM)

TargetMolReferences and Literature

1. Pachl F, et al. J Proteome Res. 2013, 12(8), 3792-3800. 2. Dumble M, et al. PLoS One. 2014, 9(6):e1200880. 3. Cheraghchi-Bashi A, et al. Oncotarget. 2015, 6(39), 41736-41749.

TargetMolCitations

1. Bing S, Xiang S, Xia Z, et al.AKT inhibitor Hu7691 induces differentiation of neuroblastoma cells.Acta Pharmaceutica Sinica B.2023

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Anti-Aging Compound Library Clinical Compound Library Neural Regeneration Compound Library Autophagy Compound Library Cancer Cell Differentiation Compound Library Glutamine Metabolism Compound Library Anti-Cancer Metabolism Compound Library

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Keywords

Uprosertib 1047634-65-0 Cytoskeletal Signaling PI3K/Akt/mTOR signaling Akt GSK2141795 GSK-2141795 GSK795 inhibit GSK 795 GSK-795 GSK 2141795 Inhibitor PKB Protein kinase B inhibitor

 

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