CC-99282
- Product Name
- CC-99282
- CAS No.
- 2379572-34-4
- Chemical Name
- CC-99282
- Synonyms
- CC-99282;golcadomide;CC-99282 ，E1212;Golcadomide (CC-99282);Golcadomide (Synonyms: CC-99282);(S)-2-(2,6-Dioxopiperidin-3-yl)-4-((2-fluoro-4-((3-morpholinoazetidin-1-yl)methyl)benzyl)amino)isoindoline-1,3-dione;2-[(3S)-2,6-dioxo-3-piperidyl]-4-[[2-fluoro-4-[(3-morpholinoazetidin-1-yl)methyl]phenyl]methylamino]isoindoline-1,3-dione
- CBNumber
- CB511959499
- Molecular Formula
- C28H30FN5O5
- Formula Weight
- 535.58
- MOL File
- 2379572-34-4.mol
CC-99282 Property
- form
- Solid
- color
- Light yellow to yellow
CC-99282 Chemical Properties,Usage,Production
Uses
Golcadomide (CC-99282) is a potent and orally active CRBN E3 ligase modulator (CELMoD). Golcadomide interacts with the CRL4 CRBN E3 ubiquitin ligase substrate receptor CRBN, inducing the recruitment and ubiquitin-mediated proteasomal degradation of the transcription factors Ikaros and Aiolos. Golcadomide shows potential for research in cancer-related fields, including chronic lymphocytic leukemia (CLL) and non-Hodgkin lymphoma (NHL)[1][2].
in vivo
Golcadomide (1 mg/kg) monotherapy results in modest tumor growth inhibition, whereas the combination of Golcadomide (1 mg/kg) and rituximab (10 mg/kg) results in tumor regression in 100% of animals in the WSU-DLCL2 model and the FL xenograft model.
IC 50
Cereblon
References
[1] J.-M. Michot, et al. A PHASE 1, MULTICENTER, OPEN-LABEL STUDY OF CC-99282 ALONE AND IN COMBINATION WITH RITUXIMAB IN PATIENTS WITH RELAPSED OR REFRACTORY NON-HODGKIN LYMPHOMAS. Hematological Oncology. Volume 39, Issue S2, Jun. 2021.
[2] Carrancio S, et al. CC-99282 is a novel cereblon (CRBN) E3 ligase modulator (CELMoD) agent with enhanced tumoricidal activity in preclinical models of lymphoma[J]. Blood, 2021, 138: 1200.
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