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HSN608

Chemical Structure : HSN608

CAS No.: 2234239-90-6

HSN608 (HSN-608, HSN 608)

Catalog No.: PC-20708Not For Human Use, Lab Use Only.

HSN608 (HSN 608) is a potent inhibitor of RET solvent-front mutants, inhibits RET G810 solvent-front mutants and the V804M gatekeeper mutant with IC50 of <50 nM in cell culture, inhibits ABL1(T315I) with IC50 of 40.7 nM.

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

    Biological Activity

    HSN608 (HSN 608) is a potent inhibitor of RET solvent-front mutants, inhibits RET G810 solvent-front mutants and the V804M gatekeeper mutant with IC50 of <50 nM in cell culture, inhibits ABL1(T315I) with IC50 of 40.7 nM.
    HSN608 inhibits selpercatinib/pralsetinib-resistant RET G810 mutants.
    HSN608 inhibits ABL1 and ABL1(T315I) activities in KCL22 and KCL22-IR cell lines.
    Oral administration of HSN608 at a well-tolerated dose (30 mg/kg) gave plasma level > 30x the IC50s of inhibiting all G810 mutants in cell culture.
    HSN608 significantly suppressed and caused regression of the selpercatinib-resistant tumors of cell-derived xenograft tumors driven by KIF5B-RET (G810C).

    Physicochemical Properties

    M.Wt 545.57
    Formula C29H26F3N7O
    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

    5-((8-amino-1,7-naphthyridin-5-yl)ethynyl)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)nicotinamide

    References

    1. Ujjwol Khatri, et al. Mol Cancer Ther. 2023 Apr 17;OF1-OF9.

    2. Elizabeth A Larocque, et al. ChemMedChem. 2018 Jun 20;13(12):1172-1180.

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