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    PHT-427 (CS-0223)
    PHT-427 (CS-0223)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0165
    CAS #: 1191951-57-1Purity ≥98%

    Description: PHT-427 (CS0223) is a novel, potent, orally bioactive and dual inhibitor of Akt and PDPK1 (PtdIns dependent protein kinase-1) with potential anticancer activity. It has high affinity binding for the pleckstrin homology (PH) domains of Akt and PDPK1 with Kis of 2.7 μM and 5.2 μM, respectively. PDPK1/Akt signaling plays a critical role in activating proliferation and survival pathways within cancer cells. In summary, PHT-427 has significant in vivo antitumor activity and minimal toxicity as a novel PH domain binding inhibitor of PDPK1/Akt signaling.

    References: Mol Cancer Ther. 2010 Mar;9(3):706-17; Cancer Res. 2009 Jun 15;69(12):5073-81.

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    Molecular Weight (MW)409.61
    CAS No.1191951-57-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 82 mg/mL (200.2 mM)
    Water: <1 mg/mL
    Ethanol: 60 mg/mL (146.5 mM)
    Solubility (In vivo)5% DMSO+95% Corn oil: 5mg/mL
    Other info

    Synonym: PHT427; PHT-427; PHT 427.

    Chemical Name: 4-dodecyl-N-(1,3,4-thiadiazol-2-yl)benzenesulfonamide


    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)


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    In Vitro

    Kinase Assay: All interaction analyses are performed with a Biacore 2000, Biacore 2000 Control Software v3.2, and BIAevaluation v4.1 analysis software. The PH domain GST-fusion proteins (Akt1, IRS1, and PDK1) are immobilized on a CM5 Sensorchip using Biacore's Amine Coupling Kit to a level of 10,000 Response units (RUs). Small molecule analytes at concentrations ranging from 0.1 to 10 × the predicted KD are injected at a high flow rate (30μL/min). DMSO concentrations in all samples and running buffer are 1% (v/v) or less. 


    Cell Assay: PH-427 is a pleckstrin homology domain inhibitor to Akt/PDPK1. PH-427 significantly reduces phospho-Ser241-PDPK1 phospho-Thr308-Akt in PC-3 prostate cancer cells at 10 μM, which shows that PHT-427 could inhibit both Akt and PDPK1. PHT-427 also inhibits translocation of the Akt and PDPK1 PH domains in plasma membrane. PHT-427 induces apoptosis and inhibits AKT phosphorylation with IC50 of 8.6 μM (in BxPC-3 cells), which mainly on its Ser473 residue and less strongly on Thr308 residue without affecting total Akt protein expression. PHT-427 also shows antiproliferation in Panc-1 cells with IC50 of 65 μM.

    In Vivo

    PHT-427 shows great antitumor activity in BxPC-3 pancreatic, MCF-7 breast and A-549 NSCL cancer xenografts. PHT-427 gives up to an 80% inhibition of tumor growth in BxPC-3 at doses of 125 to 250 mg/kg.

    Animal model

    BxPC-3, Panc-1, MiaPaCa-2, PC-3, SKOV-3, A-549 or MCF-7 cells are injected subcutaneously into the flanks of female scid mice.

    Formulation & Dosage

    Formulated in 40 to 50 mg/mL in sesame seed oil; 125-250 mg/kg; oral gavage


    [1] Meuillet EJ, et al. Mol Cancer Ther, 2010, 9(3), 706-717.[2] Moses SA, et al. Cancer Res, 2009, 69(12), 5073-5081.


    These protocols are for reference only. InvivoChem does not independently validate these methods.


    Effects of PHT-427 in cells. Cancer Res, 2009, 69(12), 5073-5081.


    Antitumor activity of PHT-427 analogs


    In vivo effects of PHT-427


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