CC-885 - Ligand for E3 Ligase - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECC-885Cat. No.: HY-101488CAS No.: 1010100-07-8分式: CHClNO分量: 440.88作靶点: Ligand for E3 Ligase作通路: PROTAC储存式: Powder -20C 3 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 67.5 mg/mL (153.10 mM; Need ultrasonic)Mass Solve

2、nt1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.2682 mL 11.3410 mL 22.6819 mL5 mM 0.4536 mL 2.2682 mL 4.5364 mL10 mM 0.2268 mL 1.1341 mL 2.2682 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在

3、您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.25 mg/mL (5.10 mM); Suspended solution; Need ultrasonic2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.25 mg/mL (5.10 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE物活性 CC-885C

4、RBN 蛋的调节剂，有潜在的抗肿瘤活性。IC50 & Target CRBN 1.体外研究 Acute myeloblatlic leukemia (AML) cell lines, human liver epithelial cell line (THLE-2) and human peripheralblood mononuclear cells (PBMC) are treated with varying concentrations of CC-885, with IC50s of 10-6-1 M.The effect of CC-885 on cell proliferatio

5、n in AML cell lines, THLE-2 and human PBMC is more powerful thanLenalidomide and Pomalidomide with IC50s10 M. To address whether the cereblon-dependent degradationof GSPT1 is responsible for the cytotoxic effects of CC-885, a GSPT1 mutant that retains its normal function,but loses CC-885-dependent c

6、ereblon binding, is used to distinguish the role of GSPT1 from that of othersubstrates. CC-885 is tested in 293T HEK cells stably expressing the CC-885-sensitive or -resistant GSPT1variants. Overexpression of a resistant variant GSPT1(1138)/(G575N) completely abrogate the CC-885-induced anti-prolife

7、ration, whereas overexpression of a CC-885-sensitive variant GSPT1(1-138) only conferpartial protection. Similar results are obtained in AML cell lines 1.PROTOCOLCell Assay 1 Human cancer cell lines cultured in the growth medium are seeded into black 384-well plates containingDMSO or test compounds

8、such as CC-885 (10-6-1 M). The seeding density for each cell line is optimizedto allow the cell growth in the linear range during a 3-day culture period. To test the compound effect on cellproliferation in acute myeloid leukaemia (AML) cell lines, 5,000 to 10,000 cells per well in 200 l completecult

9、ure 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 Assay1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Mary E. Matyskiela, et al. A novel cereblon modulator recruits GSPT1 to the CRL4CRBN ubiquitin ligase. Nature. 2016 Jul14;535(7611):252-7.McePdfHeightCaution: Product has not been fully validated f