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.
