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首页-抗体药物偶连体和PROTACs-PROTAC-MS3227
MS3227

Chemical Structure : MS3227

CAS No.:

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MS3227 (MS 3227, MS-3227)

货号: PC-49672Not For Human Use, Lab Use Only.

MS3227 is a proteolysis-targeting chimera (PROTAC) that targets MDM2 by recruiting the E3 ligase VHL, resulting in proteasome-dependent degradation of MDM2.

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

    生物&药学活性

    MS3227 is a proteolysis-targeting chimera (PROTAC) that targets MDM2 by recruiting the E3 ligase VHL, resulting in proteasome-dependent degradation of MDM2.
    In WT TP53 leukemia cell lines, MS3227 led to activation of p53 targets p21, PUMA, and MDM2 and resulted in cell-cycle arrest, apoptosis, and decreased viability.
    MS3227 also shows potent effect in primary patient specimens with selectivity towards leukemic blasts.
    MS3227 enhanced the activity of other anti-leukemic agents including azacytidine, cytarabine, and venetoclax.
    MS3227 treatment was shown to downregulate MCL-1, a known mediator of resistance to venetoclax.

    物理化学性质&存储条件

    分子量 1221.41
    分子式 C62H83Cl2N7O10S2
    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

    2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-((4-(10-(((S)-1-((2S,4R)-4-hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-10-oxodecanoyl)piperazin-1-yl)sulfonyl)-3,3-dimethylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid

    参考文献

    1. Bridget K Marcellino, et al. Leukemia. 2022 Oct 29. doi: 10.1038/s41375-022-01735-6.

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