An inhibitor of Akt and PDPK1
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PHT-427

Item No. 24188

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-dodecyl-N-1,3,4-thiadiazol-2-yl-benzenesulfonamide
CAS Number
1191951-57-1
Synonyms
  • Akt Inhibitor XIV
Molecular Formula
C20H31N3O2S2
Formula Weight
409.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 33 mg/mlDMF:PBS (pH 7.2) (1:4): 0.20 mg/mlDMSO: 16 mg/ml
λmax
226, 270 nm
SMILES
CCCCCCCCCCCCC1=CC=C(S(NC2=NN=CS2)(=O)=O)C=C1
InChi Code
InChI=1S/C20H31N3O2S2/c1-2-3-4-5-6-7-8-9-10-11-12-18-13-15-19(16-14-18)27(24,25)23-20-22-21-17-26-20/h13-17H,2-12H2,1H3,(H,22,23)
InChi Key
BYWWNRBKPCPJMG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $42

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    10 mg

    $79

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    25 mg

    $183

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    50 mg

    $343

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    Product Description

    PHT-427 is an inhibitor of the serine/threonine kinases Akt and phosphoinositide-dependent protein kinase-1 (PDPK1) with Ki values of 2.7 and 5.2 μM, respectively, that selectively binds to the pleckstrin homology binding domain of both kinases.1 PHT-427 (10 µM) inhibits PDPK1 and Akt autophosphorylation in BxPC-3 prostate cancer cells. In vivo, PHT-427 (125-250 mg/kg) reduces tumor growth in BxPC-3, Panc-1, MiaPaCa-2, PC3, SKOV3, A549, and MCF-7 xenograft mouse models, with up to 80% reduction in growth for those containing PIK3CA mutations. PHT-427 (200 mg/kg) also enhances the antitumor effect of paclitaxel (Item No. 10461) in an MCF-7 breast cancer xenograft mouse model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Meuillet, E.J., Zuohe, S., Lemos, R., et al. Molecular pharmacology and antitumor activity of PHT-427, a novel Akt/phosphatidylinositide-dependent protein kinase 1 pleckstrin homology domain inhibitor. Mol. Cancer Ther. 9(3), 706-717 (2010).