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首页-小分子抑制剂&激动剂-Others-Other Targets-Compound 30666
Compound 30666

Chemical Structure : Compound 30666

CAS No.: 426237-78-7

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Compound 30666

货号: PC-20224Not For Human Use, Lab Use Only.

Compound 30666 is a specific small molecule inhibitor of IgH enhancer transcriptional activity with IC50 of 2.1 uM, inhibits immunoglobulin production by MM cells.

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

    生物&药学活性

    Compound 30666 is a specific small molecule inhibitor of IgH enhancer transcriptional activity with IC50 of 2.1 uM, inhibits immunoglobulin production by MM cells.
    Compound 30666 does not act on other enhancer/promoter driven systems.
    Compound 30666 (5 uM) represses the expression of IgH translocation-induced oncogenes (CCND1, FGFR3/MMSET, and MYC) in MM and NHL cell lines.
    Compound 30666 exhibits selective cytotoxicity in cells positive for IgH translocations with mean EC50 of 4.0 uM, while less sensitive to IgH translocation negative cells and normal cells (EC50=51 uM).
    Compound 30666 (5 mg/kg, i.p.) exhibits favorable pharmacokinetic properties and anti-MM activity in vivo.
    Compound 30666 downregulates MYC levels in BL cell lines and alters IGH enhancer RNA expression, cuases a global decrease of H3K27ac and an increase of H3K4me1.
    Compound 30666 exhibits consistent growth inhibition in Burkitt lymphoma (BL) and diffuse large B-cell lymphoma (DLBCL).

    物理化学性质&存储条件

    分子量 342.40
    分子式 C21H18N4O
    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

    7-[[(4-methyl-2-pyridinyl)amino](2-pyridinyl)methyl]-8-quinolinol

    参考文献

    1. Nathan G Dolloff. Cancer Biol Ther. 2019;20(4):571-581.

    2. Hamdan FH, et al. Gut. 2023 Mar 8:gutjnl-2022-328154.

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