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CC-885
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CC-885图片
CAS NO:1010100-07-8
规格:98%
分子量:440.9
包装与价格:
包装价格(元)
500ug电议
1mg电议
5mg电议
10mg电议

产品介绍
CC-885 is a modulator of the E3 ligase protein cereblon with antiproliferative effects on human myeloid leukemia cell lines.
CAS:1010100-07-8
分子式:C22H21ClN4O4
分子量:440.9
纯度:98%
存储:Store at -20°C

Background:

CC-885 is a cereblon (CRBN) modulator with potent anti-tumour activity.


Acute 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].


参考文献:
[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.