常用名：CC-885

产品描述：

CC-885 is a modulator of cereblon (CRBN). It has potent anti-tumour activity.

体外活性 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. CC-885 is tested in 293T HEK cells stably expressing the CC-885-sensitive or -resistant GSPT1 variants. 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. 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. 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].

分子量 440.88

分子式 C22H21ClN4O4

CAS No. 1010100-07-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 67.5 mg/mL (153.10 mM), Sonication is recommended.

PROteolysis TArgeting Chimeras (PROTACs) 通过将靶蛋白和 E3 连接酶结合起来，从而“劫持”细胞的泛素-蛋白酶体系统（UPS）来实现蛋白质的降解。由于 PROTACs 只需具有高选择性地结合其靶标（而不是抑制靶蛋白的酶活性），目前有许多努力将先前无效的抑制剂分子改造为 PROTACs，用作下一代药物。

产地：西安

用途：科研！

厂家：西安齐岳生物科技有限公司

温馨提示：仅用于科研，不能用于人体实验！

相关产品：  

Pomalidomide-2-2-2-2-2-2-6-NH2 hydrochloride

Pomalidomide-2-2-2-2-2-2-6-alkyne

Pomalidomide-2-2-6-I

Pomalidomide-2-2-6-N3

Pomalidomide-2-2-6-acid

Pomalidomide-2-2-6-alkyne