A selective Akt inhibitor
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Uprosertib

Item No. 19904

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(1S)-2-amino-1-[(3,4-difluorophenyl)methyl]ethyl]-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-furancarboxamide
CAS Number
1047634-65-0
Synonyms
  • GSK795
  • GSK2141795
Molecular Formula
C18H16Cl2F2N4O2
Formula Weight
429.2
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 1 mg/ml
λmax
239 nm
SMILES
FC1=CC=C(C[C@@H](CN)NC(C2=CC(C3=C(Cl)C=NN3C)=C(Cl)O2)=O)C=C1F
InChi Code
InChI=1S/C18H16Cl2F2N4O2/c1-26-16(12(19)8-24-26)11-6-15(28-17(11)20)18(27)25-10(7-23)4-9-2-3-13(21)14(22)5-9/h2-3,5-6,8,10H,4,7,23H2,1H3,(H,25,27)/t10-/m0/s1
InChi Key
AXTAPYRUEKNRBA-JTQLQIEISA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $128

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    10 mg

    $236

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    25 mg

    $502

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    Product Description

    Uprosertib is a selective, orally bioavailable inhibitor of Akt (IC50s = 180, 328, and 38 nM for Akt1, Akt2, and Akt3, respectively).1 Uprosertib preferentially inhibits the proliferation of human cancer cell lines with Akt pathway activation via PI3K/PTEN mutation or loss.2 It can cause cell cycle arrest and consequent tumor growth inhibition in mice bearing either BT474 breast tumor or SKOV3 ovarian tumor xenografts.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Pachl, F., Plattner, P., Ruprecht, B., et al. Characterization of a chemical affinity probe targeting Akt kinases. J. Proteome Res. 12(8), 3792-3800 (2013).

    2. Dumble, M., Crouthamel, M.C., Zhang, S.Y., et al. Discovery of novel AKT inhibitors with enhanced anti-tumor effects in combination with the MEK inhibitor. PLoS One 9(6), e100880 (2014).