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首页-小分子抑制剂&激动剂-Wnt/Notch/Hedgehog-Notch-CAD204520
CAD204520

Chemical Structure : CAD204520

CAS No.: 2682205-21-4

CAD204520 (CAD 204520)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    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.

    物理化学性质&存储条件

    分子量 512.439
    分子式 C23H34Cl2F3N3O2
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    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

    参考文献

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

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