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IC5150 CC-885 抑制剂/拮抗剂/激动剂 索莱宝

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  • ¥890 - 4190
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  • 北京
  • IC5150
  • 2025年07月23日
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    • 详细信息
    • 文献和实验
    • 技术资料
    • 保存条件

      Powder:-20℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year

    • 保质期

      Powder:-20℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year

    • 英文名

      CC-885

    • 库存

      现询

    • 供应商

      北京索莱宝科技有限公司

    • CAS号

      1010100-07-8

    • 规格

      50mg/25mg/10mg/5mg

    规格:50mg产品价格:¥4190.0
    规格:25mg产品价格:¥2790.0
    规格:10mg产品价格:¥1290.0
    规格:5mg产品价格:¥890.0

    基本信息
    CASNo.1010100-07-8
    英文名称CC-885
    分子式C22H21ClN4O4
    分子量440.88
    溶解性Soluble in DMSO ≥5mg/mL
    纯度≥98%
    外观(性状)Solid
    储存条件Powder:-20℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
    MDLMFCD31657329
    SMILESCC1=C(C=C(C=C1)NC(=O)NCC2=CC3=C(C=C2)C(=O)N(C3)C4CCC(=O)NC4=O)Cl
    InChIKeyCC1=C(C=C(C=C1)NC(=O)NCC2=CC3=C(C=C2)C(=O)N(C3)C4CCC(=O)NC4=O)Cl
    InChIInChI=1S/C22H21ClN4O4/c1-12-2-4-15(9-17(12)23)25-22(31)24-10-13-3-5-16-14(8-13) 11-27(21(16)30)18-6-7-19(28)26-20(18)29/h2-5,8-9,18H,6-7,10-11H2,1H3,(H2 ,24,25,31)(H,26,28,29)
    PubChem CID24788636
    靶点CRBN
    通路Ubiquitin
    背景说明CC-885 是 CRBN 蛋白的调节剂。
    生物活性CC-885 is a cereblon (CRBN) modulator with potent anti-tumour activity.[1]
    In VitroAcute myeloblatlic leukemia(AML)cell lines,human liver epithelial cell line(THLE-2)and human peripheral blood mononuclear cells(PBMC)are treated with varying concentrations of CC-885,with IC50s of 10×-6-1 μM. The effect of CC-885 on cell proliferation in AML cell lines,THLE-2 and human PBMC is more powerful than Lenalidomide and Pomalidomide with IC50s>10 μM. To address whether the cereblon-dependent degradation of GSPT1 is responsible for the cytotoxic effects of CC-885,a GSPT1 mutant that retains its normal function,but loses CC-885-dependent cereblon binding,is used to distinguish the role of GSPT1 from that of other substrates. CC-885 is tested in 293T HEK cells stably expressing the CC-885-sensitive or -resistant GSPT1 variants. Overexpression of a resistant variant GSPT1Δ(1–138)/(G575N)completely abrogate the CC-885-induced anti-proliferation,whereas overexpression of a CC-885-sensitive variant GSPT1Δ(1-138)only confer partial protection. Similar results are obtained in AML cell lines[1].
    细胞实验Human cancer cell lines cultured in the growth medium are seeded into black 384-well plates containing DMSO or test compounds such as CC-885(10×-6-1 μM). The seeding density for each cell line is optimized to allow the cell growth in the linear range during a 3-day culture period. To test the compound effect on cell proliferation in acute myeloid leukaemia(AML)cell lines,5,000 to 10,000 cells per well in 200 μl complete culture media are seeded into black 96-well plates containing DMSO or test compounds such as CC-885. After 48 or 72 h,cell proliferation is assessed using the CellTiter-Glo(CTG)Luminescent Cell Viability Assay[1].
    数据来源文献[1]. Mary E. Matyskiela, et al. A novel cereblon modulator recruits GSPT1 to the CRL4CRBN ubiquitin ligase. Nature. 2016 Jul 14;535(7611):252-7.
    单位

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