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CAD204520

Chemical Structure : CAD204520

CAS No.: 2682205-21-4

CAD204520 (CAD 204520)

Catalog No.: PC-38269Not For Human Use, Lab Use Only.

CAD204520 (CAD 204520) is a potent, specific, orally available inhibitor of SERCA (Sarco/Endoplasmic Reticulum Calcium ATPase) with IC50 of 0.34 uM.

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    Biological Activity

    CAD204520 (CAD 204520) is a potent, specific, orally available inhibitor of SERCA (Sarco/Endoplasmic Reticulum Calcium ATPase) with IC50 of 0.34 uM.
    CAD204520 preferentially targets mutated over wild-type NOTCH1 proteins in T-All and MCL.
    CAD204520 preferentially inhibited the Ca2+-ATPase by reducing SERCA's ATP hydrolysis activity with an IC50=0.34 uM as compared to the Na+/K+-ATPase (IC50, 8.30 uM) and the H+-ATPase.
    CAD204520 modulates Notch1 signaling, and preferentially inhibits NOTCH1 mutated cancers.
    CAD204520 suppresses NOTCH1-mutated leukemic cells in a T-ALL xenografted model without causing cardiac toxicity.

    Physicochemical Properties

    M.Wt 512.439
    Formula C23H34Cl2F3N3O2
    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

    4-(2-(2-(3-propyl-6-(trifluoromethoxy)-1H-indol-2-yl)piperidin-1-yl)ethyl)morpholine dihydrochloride

    References

    1. Marchesini M, et al. Cell Chem Biol. 2020 Jun 18;27(6):678-697.e13. 

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