Iberdomide-CC-220-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEIberdomideCat. No.: HY-101291CAS No.: 1323403-33-3Synonyms: CC-220分式: CHNO分量: 449.5作靶點(diǎn): Ligand for E3 Ligase作通路: PROTAC儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 30 mg/mL (66.74 mM)* m

2、eans soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.2247 mL 11.1235 mL 22.2469 mL5 mM 0.4449 mL 2.2247 mL 4.4494 mL10 mM 0.2225 mL 1.1123 mL 2.2247 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Iberdomide (CC-220)是cereblon (CRBN) 調(diào)節(jié)劑，IC50為

3、60 nM。體外研究 Iberdomide contains a glutarimide ring that binds in the try-tryptophan pocket of cereblon and anisoindolinone ring that can interact with both cereblon and substrates. Treatment with Iberdomide results inthe loss of Ikaros and Aiolos protein levels with EC50s of 1 nM and 0.5 nM 1.1/2 Mas

4、ter of Small Molecules 您邊的抑制劑師www.MedChemE體內(nèi)研究 Iberdomide (CC-220) is currently in phase 2 clinical trials for the treatment of systematic lupus erythematosus(SLE) and phase 1b/2a clinical trials for relapsed and refractory multiple myeloma (MM) 1.PROTOCOLKinase Assay 1 Iberdomide is dissolved in DM

5、SO. In the assay, 60 nM 6Xhis-tagged CRBN-DDB1 is combined with 30 nMcy5-conjugated cereblon modulator and 3 nM LanthaScreen Eu-anti-His Tag antibody in 20 mM HEPES pH7, 150 mM NaCl, 0.005% Tween-20 assay buffer. FRET is observed by exciting at 340 nm and monitoringemission at 615 nm and 665 nm, and

6、 FRET efficiency is determined by the ratio of FRET to non-FRETemission. Competing cereblon modulating compound (Iberdomide) or DMSO carrier is titrated and incubatedfor 10 min before scanning 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研

7、獻(xiàn) Blood Cancer J. 2019 Feb 11;9(2):19. Elife. 2018 Aug 1;7. pii: e38430.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Matyskiela ME, et al. A Cereblon Modulator (CC-220) with Improved Degradation of Ikaros and Aiolos. J Med Chem. 2017 Apr 20.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use