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    ETP-46321
    ETP-46321

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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 #: V2910
    CAS #: 1252594-99-2Purity ≥98%

    Description: ETP-46321 is a novel, potent and orally bioavailable inhibitor of PI3Kα and PI3Kδ with Kiapp values of 2.3 nM and 14.2 nM, respectively in biochemical assays. PI3K is an important target for cancer therapeutics due to the deregulation of this signaling pathway in a wide variety of human cancers. TP-46321 PK/PD studies showed time dependent downregulation of AKT(Ser473) phosphorylation, which correlates with compound levels in tumor tissue and demonstrating to be efficacious in a GEMM mouse tumor model driven by a K-Ras(G12V) oncogenic mutation. Treatment with ETP-46321 resulted in significant tumor growth inhibition.

    References:  2012 May 15;22(10):3460-6.


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    Molecular Weight (MW) 473.55 
    Formula C20H27N9O3S                 
    CAS No. 1252594-99-2                 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: ≥ 33 mg/mL
    Water: <1 mg/mL
    Ethanol: 
    SMILES Code NC1=NC=C(C2=CN3C(C(N4CCOCC4)=N2)=NC(CN5CCN(S(=O)(C)=O)CC5)=C3)C=N1
    Synonyms ETP46321; ETP-46321; ETP 46321


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    In Vitro

    In vitro activity: ETP-46321 is a novel, potent and orally bioavailable inhibitor of PI3Kα and PI3Kδ with Kiapp values of 2.3 nM and 14.2 nM, respectively in biochemical assays. PI3K is an important target for cancer therapeutics due to the deregulation of this signaling pathway in a wide variety of human cancers. TP-46321 PK/PD studies showed time dependent downregulation of AKT(Ser473) phosphorylation, which correlates with compound levels in tumor tissue and demonstrating to be efficacious in a GEMM mouse tumor model driven by a K-Ras(G12V) oncogenic mutation. Treatment with ETP-46321 resulted in significant tumor growth inhibition. 


    Kinase Assay: ETP-46321 is selected to be screened against other PI3K isoforms. ETP-46321 is more potent against isoform α (Kiapp=2.3 nM). ETP-4632, has been profiled and shown to be a potent PI3K α and δ inhibitor, highly selective versus mTOR and 288 representative kinases. ETP-46321 is also tested against three of the p110α mutant enzymes detected in human cancers (E542K, E545K and H1047R), being equipotent against these mutants when compared to the wild type protein (Kiapp=2.33, 1.77 and 1.89 nM for PI3Kα-H1047R, PI3Kα-E545K and PI3Kα-E542K, respectively). ETP-46321 inhibits the phosphorilation of AKT in U2OS cell line with an IC50 of 8.3 nM.


    Cell Assay: 

    In VivoETP-46321 was selected for in vivo studies based on its appealing pharmacokinetic profile in BALB-C mice, low in vivo Clearance (0.6 L/h/Kg) and good oral bioavailability (90%). ETP-46321 demonstrates a good pharmacokinetic profile in mice and is selected for preliminary in vivo evaluation in a lung tumor mouse model driven by a K-RasG12V oncogenic mutation, showing significant tumor growth inhibition, and reduction of the tumor metabolic activity as measured by positron emission tomography (PET) techniques
    Animal model Mouse with lung tumor model driven by a K-RasG12V oncogenic mutation
    Formulation & Dosage
    References  2012 May 15;22(10):3460-6.


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

    ETP-46321

     2012 May 15;22(10):3460-6.




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