Cat. No. Name Size Price Add Cart
KI0440PHT-42710 mg$56
PHT-42750 mg$235
PHT-427200 mg$650

Chemical Characteristic

Product NamePHT-427
CAS No.1191951-57-1
Molecular Weight 409.62
Chemical Name4-Dodecyl-N-1,3,4-thiadiazol-2-ylbenzenesulfonamide
Chemical Structure

Biological activities

PHT-427 is a novel AKT/PDPK1 pleckstrin homology domain inhibitor. PHT-427 binds to not only the pleckstrin homology (PH) binding domain of signaling molecules in cancer, but also the PH domain of PDPK1. PHT-427 prevents Akt and PDKP1 signaling and their downstream targets in sensitive but not resistant cells and tumor xenografts. PHT-427 slightly increases the PDPK1-independent phospho-Ser473-Akt. The IC50 of PHT-427 for cell growth inhibition is around 30 µM. [1] When administrated orally, PHT-427 prevents the proliferation of human tumor xenografts in immunodeficient mice with up to 80% suppression in the most sensitive tumors. Prevention of PDKP1 by PHT-427 is more closely correlated to antitumor effects than Akt suppression. Combinations of PHT-427 plus paclitaxel and erlotinib have greater than additive antitumor activity in breast cancer and non small cell lung cancer (NSCLC). When administrated over 5 days PHT-427 induces no weight loss or change in blood chemistry.[1]


[1] Meuillet EJ, 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. 2010, 9(3): 706-717.

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