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    ONO-4059 analogue
    ONO-4059 analogue

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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 #: V0649
    CAS #: 1351635-67-0 Purity ≥98%

    Description: ONO-4059 analogue, an analogue of ONO-4059, is a novel, covalent, selective and orally bioavailable BTK inhibitor with potential anticancer and anti-inflammatory activity. It inhibits BTK with IC50 of 23.9 nM. ONO-4059 has demonstrated high antitumor activity in several pre-clinical models. It potently and dose-dependently reverse clinical arthritis and prevented bone damage in the CIA model. ONO-4059 inhibited the TMD-8 cell growth and Btk phosphorylation in a concentration-dependent manner. Furthermore, the decrease in Btk phosphorylation subsequently down-regulated Erk phosphorylation. After the combination of ONO-4059 with doxorubicin, etoposide, vincristine and dexamethasone, increased apoptosis ratio was observed, 25, 20, 17 and 29%, respectively.

    References: Blood. 2016 Jan 28;127(4):411-9.

    Related CAS: 1439901-97-9 (HCl); 1351635-67-0 (ONO-4059-analog); 1351636-18-4 (free base)  

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    Molecular Weight (MW)456.50
    FormulaC25H24N6O3
    CAS No.1351635-67-0 (ONO-4059-analog); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 20 mg/mL (43.8 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other infoChemical Name: (S)-9-(1-acryloylpiperidin-3-yl)-6-amino-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one
    InChi Key: KSUDUUBCXJUFRL-SFHVURJKSA-N
    InChi Code: InChI=1S/C25H24N6O3/c1-2-21(32)29-14-6-7-18(15-29)31-24-22(23(26)27-16-28-24)30(25(31)33)17-10-12-20(13-11-17)34-19-8-4-3-5-9-19/h2-5,8-13,16,18H,1,6-7,14-15H2,(H2,26,27,28)/t18-/m0/s1
    SMILES Code: O=C1N(C2=CC=C(C=C2)OC3=CC=CC=C3)C4=C(N)N=CN=C4N1[[email protected]@H]5CN(C(C=C)=O)CCC5
    SynonymsONO 4059-Analog; ONO-4059-Analog; ONO-WG-307; ONO4059-Analog; GS 4059-Analog; GS-4059-Analog; GS4059-Analog.


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    In Vitro

    In vitro activity: In TMD-8 cells, ONO-4059 inhibits cell growth with IC50 of 3.59 nM, and induces cell apoptosis. The combination of of ONO-4059 with doxorubicin, etoposide, vincristine or dexamethasone causes the increased apoptosis ratio.


    Kinase Assay: ONO-4059 analog is the analog of ONO-4059, ONO-4059 is a highly potent and selective Btk inhibitor. IC50 value: sub-nM range.


    Cell Assay: ONO-4059 inhibited the TMD-8 cell growth and Btk phosphorylation in a concentration-dependent manner. Furthermore, the decrease in Btk phosphorylation subsequently down-regulated Erk phosphorylation. After the combination of ONO-4059 with doxorubicin, etoposide, vincristine and dexamethasone, increased apoptosis ratio was observed, 25, 20, 17 and 29%, respectively.

    In VivoFor the 100-200 mm3 tumour groups, tumour growth inhibition at the final treatment day was 23% in QD, 72.9% in BD and 100% in dose mixed in food, groups respectively. For the 400-450 mm3 tumour groups, no growth inhibition was observed in the QD group and, growth inhibitions of 27.5% in BD and 100% in dose mixed in food were observed. The PK concentration and phosphorylated Btk inhibition levels of those animals whose dose was mixed in with food were higher than that of other treatment groups.
    Animal modelMouse tumor and CIA models
    Formulation & DosageONO-4059 has demonstrated anti-tumour activity in several pre-clinical models. ONO-4059 potently and dose-dependently reverse clinical arthritis and prevented bone damage in the CIA model
    ReferencesBlood. 2016 Jan 28;127(4):411-9.


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

    ONO-4059 analogue

    Efficacy of ONO/GS-4059 in patients with DLBCL. Blood. 2016 Jan 28;127(4):411-9.

    ONO-4059 analogue

    Efficacy of ONO/GS-4059 in patients with CLL. Blood. 2016 Jan 28;127(4):411-9.

    ONO-4059 analogue

    Efficacy of ONO/GS-4059 in patients with MCL. Blood. 2016 Jan 28;127(4):411-9.


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