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MedChemExpressModel Golcadomide -2379572-34-4

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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].
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Golcadomide

MCE China:Golcadomide

Brand:MedChemExpress (MCE)

Cat. No.HY-146237

CAS:2379572-34-4

Synonyms:CC-99282

Purity:97.01%

Storage:Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month

Shipping:Room temperature in continental US; may vary elsewhere.

Description: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).

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.

IC50 & Target:Cereblon

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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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