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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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Purity & Documentation Purity: >98% (HPLC)

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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