CC-885 is a potent Cereblon Modulator with potent antitumor activity mediated through the degradation of GSPT1. was demonstrated to mediate antitumor effects through the recruitment and degradation of G1 to S phase transition 1 protein (GSPT1). GSPT1 (also named eRF3a) is a translation termination factor that binds eukaryotic translation termination factor 1 (eFR1) to mediate stop codon recognition and nascent protein release from the ribosome.
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Name | CC-885 |
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Iupac Chemical Name | N-(3-chloro-4-methylphenyl)-n'-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1-oxo-1h-isoindol-5-yl]methyl]-urea |
Synonyms | CC-885, CC 885, CC885. |
Molecular Formula | C22H21ClN4O4 |
Molecular Weight | 440.88 |
Smile | ClC=1C=C(C=CC1C)NC(=O)NCC=1C=C2CN(C(C2=CC1)=O)C1C(NC(CC1)=O)=O |
InChiKey | DOEVCIHTTTYVCC-UHFFFAOYSA-N |
InChi | InChI=1S/C22H21ClN4O4/c1-12-2-4-15(9-17(12)23)25-22(31)24-10-13-3-5-16-14(8-13)11-27(21(16)30)18-6-7-19(28)26-20(18)29/h2-5,8-9,18H,6-7,10-11H2,1H3,(H2,24,25,31)(H,26,28,29) |
CAS Number | 1010100-07-8 |
Related CAS |
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Formulation | Off white to light purple solid powder |
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Purity | 98% Min. |
Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
Solubility | Soluble in DMSO |
Handling | |
Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
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Clinical study |
1: Matyskiela ME, Lu G, Ito T, Pagarigan B, Lu CC, Miller K, Fang W, Wang NY,
Nguyen D, Houston J, Carmel G, Tran T, Riley M, Nosaka L, Lander GC, Gaidarova S,
Xu S, Ruchelman AL, Handa H, Carmichael J, Daniel TO, Cathers BE, Lopez-Girona A,
Chamberlain PP. A novel cereblon modulator recruits GSPT1 to the CRL4(CRBN)
ubiquitin ligase. Nature. 2016 Jul 14;535(7611):252-7. doi: 10.1038/nature18611.
Epub 2016 Jun 22. PubMed PMID: 27338790.
2: The Cereblon Modulator CC-885 Exhibits Antitumor Activity. Cancer Discov. 2016
Aug;6(8):OF15. doi: 10.1158/2159-8290.CD-RW2016-123. Epub 2016 Jul 1. PubMed
PMID: 27369046.
3: Hansen JD, Condroski K, Correa M, Muller G, Man HW, Ruchelman A, Zhang W,
Vocanson F, Crea T, Liu W, Lu G, Baculi F, LeBrun L, Mahmoudi A, Carmel G,
Hickman M, Lu CC. Protein Degradation via CRL4(CRBN) Ubiquitin Ligase: Discovery
and Structure-Activity Relationships of Novel Glutarimide Analogs That Promote
Degradation of Aiolos and/or GSPT1. J Med Chem. 2017 Apr 13. doi:
10.1021/acs.jmedchem.6b01911. [Epub ahead of print] PubMed PMID: 28358507.