1. PI3K/Akt/mTOR
  2. Akt
  3. Uprosertib

Uprosertib (Synonyms: GSK2141795)

Cat. No.: HY-15965 Purity: 99.85%
Handling Instructions

Uprosertib (GSK2141795) is a potent and selective pan-Akt inhibitor with IC50 values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.

For research use only. We do not sell to patients.

Uprosertib Chemical Structure

Uprosertib Chemical Structure

CAS No. : 1047634-65-0

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 636 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1056 In-stock
Estimated Time of Arrival: December 31
200 mg USD 1860 In-stock
Estimated Time of Arrival: December 31
500 mg   Get quote  
1 g   Get quote  

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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of Uprosertib:

Top Publications Citing Use of Products

    Uprosertib purchased from MCE. Usage Cited in: Mol Cancer Ther. 2017 Apr;16(4):614-624.

    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).

    Uprosertib purchased from MCE. Usage Cited in: Nat Commun. 2017 Sep 4;8(1):410.

    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.

    Uprosertib purchased from MCE. Usage Cited in: Oncotarget. 2018 Jul 31;9(59):31549-31558.

    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.

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    • Technical Information

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    • References

    Description

    Uprosertib (GSK2141795) is a potent and selective pan-Akt inhibitor with IC50 values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.

    IC50 & Target

    Akt3

    38 nM (IC50)

    Akt1

    180 nM (IC50)

    Akt2

    328 nM (IC50)

    ROCK1

    1570 nM (IC50)

    ROCK2

    1850 nM (IC50)

    CDK7

    2100 nM (IC50)

    In Vitro

    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].

    Clinical Trial
    Storage

    -20°C, stored under nitrogen

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 150 mg/mL (349.45 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3296 mL 11.6482 mL 23.2964 mL
    5 mM 0.4659 mL 2.3296 mL 4.6593 mL
    10 mM 0.2330 mL 1.1648 mL 2.3296 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      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

    • 2.

      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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Molecular Weight

    429.25

    Formula

    C₁₈H₁₆Cl₂F₂N₄O₂

    CAS No.

    1047634-65-0

    SMILES

    O=C(C1=CC(C2=C(Cl)C=NN2C)=C(Cl)O1)N[[email protected]@H](CC3=CC=C(F)C(F)=C3)CN

    Shipping

    Room temperature in continental US; may vary elsewhere

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    Product Name:
    Uprosertib
    Cat. No.:
    HY-15965
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    Uprosertib

    Cat. No.: HY-15965