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533557 AKT Inhibitor XXIII, Isozyme-Selective, GSK2141795 - CAS 1047634-65-0 - Calbiochem

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      OverviewA cell-permeable, orally available, and non-toxic pyrazolylfuran-carboxamide derived compound that acts as a highly potent, ATP-competitive, and reversible inhibitor of Akt1, Akt2, Akt3 (IC50 = 66 pM, 1.4 nM, and 1.5 nM, respectively). Shown to block the phosphorylation of multiple Akt substrates. Also shown to be a highly effective inhibitor of E17K mutant form of Akt1 (IC50 = 200 pM). Inhibits the activity of PKA, PKG1α, and PKG1β (IC50 = 2, <1, and <1 nM, respectively), but shows high selectivity over a wide panel of other protein kinases. Modestly inhibits several PKC isozymes at much higher concentrations (IC50 = 90 nM). Induces cell cycle arrest at G1 phase and causes apoptosis in BT474, LNCaP, A3, and 19.2 cell lines (~ 1 µM). Suppresses the growth of BT474 xenograft tumors in mice (98% at 30 mg/kg; 57% at 20 mg/kg, p.o. q.d x 21 days). Also induces a transient increase in blood glucose and corresponding insulin levels (200 mg/dl and 188 ng/ml, respectively with a single dose of 30 mg/kg).

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
      Catalogue Number533557
      Brand Family Calbiochem®
      SynonymsGSK 2141795, Uprosertib
      ReferencesDumble, M., et al. 2014. PLoS One. 9, e100880.
      Product Information
      CAS number1047634-65-0
      FormOff-white solid
      Hill FormulaC₁₈H₁₆Cl₂F₂N₄O₂
      Chemical formulaC₁₈H₁₆Cl₂F₂N₄O₂
      Quality LevelMQ100
      Biological Information
      Primary TargetAkt1
      Secondary targetAkt2, Akt3
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information


      AKT Inhibitor XXIII, Isozyme-Selective, GSK2141795 - CAS 1047634-65-0 - Calbiochem SDS


      Safety Data Sheet (SDS) 


      Reference overview
      Dumble, M., et al. 2014. PLoS One. 9, e100880.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision20-November-2015 JSW
      SynonymsGSK 2141795, Uprosertib
      DescriptionA cell-permeable pyrazolylfuran-carboxamide derived compound that is reported to inhibit Akt kinase activity in a reversible, ATP-competitive, and Akt1-selective manner (Ki = 0.066 nM/Akt1, 1.4 nM/Akt2, 1.5 nM/Akt3) with additional inhibitory activity against PKA & PKG (IC50 = 2.0 nM/PKA and <1 nM/PKG1α & PKG1β), while exhibiting much reduced potency toward p70S6K, ROCK, RSK1 (IC50 = 50, 126, 200 nM, respectively), and 11 PKC isoforms (IC50 in nM = 49/η, 56/β1, 64/θ, 69/δ, 86/β2, 200/γ, 690/μ, >1000/α, ε, ι, & ζ). Shown to inhibit cellular phosphorylation levels of Akt substrates, including GSK-3β Thr9, PRAS40 Thr246 (IC50 in nM against pGSK-3&beta/pPRAS40 = 34/55 in LNCaP and 143/39 in BT474 cells post 1 h drug treatment), Caspase-9 Ser196, and FOXO Thr24/32, effectively inducing FOXO nuclear localization (EC50 = 47 nM toward GFP-FOXO3a nuclear localization in MDA-MG-468 post 1 h drug treatment) without affecting MEK Ser217/221 or ERK Tyr204 phosphorylation even at 10 µM concentration. Cancer panel antiproliferation study reveals many GSK2141795-sensitive cell lines (IC50 <1 µM by viability assay based on cellular ATP content post 3-day drug treatment) contain PI3K or PTEN alternations, while many resistant lines (IC50 >1 µM) contain BRAF, KRAS, or NRAS mutations. Shown to suppress human breast carcinoma BT474 & ovarian carcinoma SKOV3 tumor growth in mice (%suppression/dose/cancer = 57/20 mg kg-1/BT474, 98/30 mg kg-1/BT474, 85/20 mg kg-1/SKOV3, 93/30 mg kg-1/SKOV3 following 21 daily oral dosages) in vivo with good tumor tissue drug exposure and concomitant tumor PRAS40 phosphorylation reduction (63% pPRAS40 reduction 2 h post 7 daily 30 mg kg-1 oral dosages; [drug] = 1.6 µg/mL plasma & 12.6 µg/mg BT474 tumor), while, unlike many other Akt inhibitors, displaying much reduced perturbation of glucose homeostasis. Effective suppression of pancreatic adenocarcinoma is demonstrated with combined GSK2141795 & MEK inhibitor treatment of mice bearing HPAC or Capan-2 tumor.
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1047634-65-0
      Chemical formulaC₁₈H₁₆Cl₂F₂N₄O₂
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesDumble, M., et al. 2014. PLoS One. 9, e100880.