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SBI-4668

Chemical Structure : SBI-4668

CAS No.: 2929401-68-1

SBI-4668 (SBI-668, SBI 4668)

Catalog No.: PC-38184Not For Human Use, Lab Use Only.

SBI-4668 (SBI-668) is a novel furanylbenzamide molecule inhibitor of both WT and oncogenic SHP2 with IC50 of 0.73/1.8 uM for Wt SHP2/SHP2-E76K, 13-fold selective over PTP1B and 73-fold selective over STEP.

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    Biological Activity

    SBI-4668 (SBI-668) is a novel furanylbenzamide molecule inhibitor of both WT and oncogenic SHP2 with IC50 of 0.73/1.8 uM for Wt SHP2/SHP2-E76K, 13-fold selective over PTP1B and 73-fold selective over STEP.
    SBI-4668 exhibited cell viability inhibitory effect on cell growth in both Kasumi-1 cells (IC50=8.5 uM) and KYSE-520 cells (IC50=5.4 uM), SBI-4668 on cell viability was also determined in additional AML cell lines, including MOLM-13 (IC50 = 12 μM) and MV4-11 (IC50 = 8.2 μM).
    SBI-4668 inhibited U-937 cell (harbor a G60R oncogenic mutation in SHP2) growth with IC50 of 6.3 uM, which is comparable to the potency found in AML cells expressing WT SHP2, while RMC4550 showed a very weak effect on this G60R mutation cell.

    Physicochemical Properties

    M.Wt 439.485
    Formula C26H17NO4S
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 1 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    (Z)-2-hydroxy-5-(5-((3-oxobenzo[b]thiophen-2(3H)-ylidene)methyl)furan-2-yl)-N-phenylbenzamide

    References

    1. Raveendra-Panickar D, et al. J Biol Chem. 2022 Jan;298(1):101477.

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