CC-99282
- Product Name
- CC-99282
- CAS No.
- 2379572-34-4
- Chemical Name
- CC-99282
- Synonyms
- CC-99282;BMS986369;BMS-986369;BMS 986369;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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P501Dispose of contents/container to..…
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.
CC-99282 Preparation Products And Raw materials
Raw materials
Preparation Products
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