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首页-抗体药物偶连体和PROTACs-PROTAC-TMX-2172
TMX-2172

Chemical Structure : TMX-2172

CAS No.: 2488892-09-5

TMX-2172 (TMX2172)

货号: PC-21526Not For Human Use, Lab Use Only.

TMX-2172 is a potent, selective CDK2 and CDK5 dual PROTAC degrader with IC50 of 6.5 nM and 6.8 nM for CDK2/cyclin A and CDK5/p25, respectively.

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

    生物&药学活性

    TMX-2172 is a potent, selective CDK2 and CDK5 dual PROTAC degrader with IC50 of 6.5 nM and 6.8 nM for CDK2/cyclin A and CDK5/p25, respectively.
    TMX-2172 shows high degradation selectivity for CDK2 and CDK5 over other cell cycle CDKs (CDK1, CDK4, and CDK6) and transcriptional CDKs (CDK7 and CDK9).
    TMX-2172 exhibits antiproliferative activity against OVCAR8 with IC50 of 33.1 nM, an ovarian cancer cell line that overexpresses CCNE1 (a well-established activator of CDK2).
    TMX-2172 exhibits an IC50 of 46.9 nM in cellular CRBN engagement assays.
    TMX-2172 induced CDK2 degradation at a concentration of 250 nM in Jurkat cells with no effect against other cell cycle CDKs.

    物理化学性质&存储条件

    分子量 970.83
    分子式 C41H45BrFN9O11S
    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-((5-bromo-2-((4-(N-(14-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-3,6,9,12-tetraoxatetradecyl)sulfamoyl)-2-methylphenyl)amino)pyrimidin-4-yl)amino)-6-fluorobenzamide

    参考文献

    1. Teng M, et al. Angew Chem Int Ed Engl. 2020 Aug 10;59(33):13865-13870.

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