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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名称 | CC-885 |
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Iupac 化学名称 | N-(3-chloro-4-methylphenyl)-n'-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1-oxo-1h-isoindol-5-yl]methyl]-urea |
同义词 | CC-885, CC 885, CC885. |
英文同义词 | CC-885, CC 885, CC885. |
分子式 | C22H21ClN4O4 |
分子量 | 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号 | 1010100-07-8 |
相关CAS号 |
包装 | 价格 | 库存 | 纯度 | 备货期 |
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大货 | 询价 | 询价 | 询价 |
外观性状 | 灰白色至浅紫色固体粉末 |
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纯度 | 98% Min. |
存储 | 干燥、黑暗,短期(日至周)0-4摄氏度,长期(月至年)0-20摄氏度。 |
可溶性 | 可溶于DMSO |
处理方式 | |
运输条件 | 作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周。 |
海关编码 |
Targets | |
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Mechanism | |
Cell study | |
Animal study | |
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.