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    BGB-102
    BGB-102

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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 #: V4519
    CAS #: 807640-87-5 (free base)Purity ≥98%

    Description: JNJ-26483327 (also known as BGB102 and BGB-102) is a novel, potent, reversible and orally bioavailable small-molecule multitargeted tyrosine kinase inhibitor against EGFR, HER2, and HER4 with IC50s of 9.6 nM, 18 nM and 40.3 nM, respectively. It has potential antineoplastic activity. JNJ-26483327 binds to and inhibits several members of the epidermal growth factor receptor (EGFR) family, including EGFR, HER2 and HER4; Src family kinases (Lyn, Yes, Fyn, Lck and Src); and vascular endothelial growth factor receptor type 3 (VEGFR3).

    References:  2010 Dec 21;8(12):e1000563.

    Related CAS : 807640-87-5 (free base); 1021686-80-5 (2HBr)   

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    BGB-102

    Name: JNJ-26483327
    CAS#: 807640-87-5 (free base)
    Chemical Formula: C22H25BrN4O2
    Exact Mass: 456.11609
    Molecular Weight: 457.3635
    Elemental Analysis: C, 57.77; H, 5.51; Br, 17.47; N, 12.25; O, 7.00
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Technical InformationSynonym: JNJ26483327; JNJ 26483327; JNJ-26483327; BGB102; BGB-102; BGB 102.
    IUPAC/Chemical Name: 35-bromo-17-methoxy-5-methyl-11-oxa-2,5-diaza-1(4,6)-quinazolina-3(1,2)-benzenacycloundecaphane
    InChi Key: JXDYOSVKVSQGJM-UHFFFAOYSA-N
    InChi Code: InChI=1S/C22H25BrN4O2/c1-27-8-4-3-5-9-29-21-11-17-19(12-20(21)28-2)24-14-25-22(17)26-18-10-16(23)7-6-15(18)13-27/h6-7,10-12,14H,3-5,8-9,13H2,1-2H3,(H,24,25,26)
    SMILES Code: CN1CCCCCOC(C(OC)=C2)=CC3=C2N=CN=C3NC4=CC(Br)=CC=C4C1


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    BGB-102


    Herceptin induces the activation of HER receptors and their dimerisation with HER2 as a result of an up-regulation and the release of HER ligands.

     BGB-102


    nhibiting PKB phosphorylation by a PKB inhibitor induces up-regulation of heregulin and ADAM17.  2010 Dec 21;8(12):e1000563.

     BGB-102


    Combination of Herceptin with ADAM inhibitors decreases HER2 phosphorylation and is additive in cell viability inhibition. 2010 Dec 21;8(12):e1000563.


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