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BIBU1361

Chemical Structure : BIBU1361

CAS No.: 793726-84-8

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BIBU1361 (BIBU 1361, BIBU-1361 )

Catalog No.: PC-62998Not For Human Use, Lab Use Only.

BIBU1361 is a potent, selective, orally active EGFR inhibitor with IC50 of 3 nM, shows weak activity against HER2 (IC50=280 nM) and no inhibition on IGF1R, HGFR, Src, and VEGFR2 (IC50>10 uM).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    BIBU1361 is a potent, selective, orally active EGFR inhibitor with IC50 of 3 nM, shows weak activity against HER2 (IC50=280 nM) and no inhibition on IGF1R, HGFR, Src, and VEGFR2 (IC50>10 uM)。
    BIBU1361 inhibits EGF-induced phosphorylation of EGFR in a dose-dependent manner in A431 cells (EC50=122 nM)。
    BIBU1361 demonstrates effectivity in tumour xenografts mice.

    Physicochemical Properties

    M.Wt 443.955
    Formula C22H27ClFN7
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    N-(3-Chloro-4-fluorophenyl)-6-[4-[(diethylamino)methyl]-1-piperidinyl]-pyrimido[5,4-d]pyrimidin-4-amine

    References

    1. Solca FF, et al. J Pharmacol Exp Ther. 2004 Nov;311(2):502-9.

    2. Ghildiyal R, et al. Mol Carcinog. 2013 Dec;52(12):970-82.

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