MGD-28 is a potent molecular glue degrader that demonstrates significant in vitro efficacy against various hematological cancer cell lines. It induces degradation of Ikaros family zinc finger proteins 1, 2, and 3 (IKZF1/2/3) and casein kinase 1 alpha (CK1α) with nanomolar potency via a Cullin-cereblon (CRBN) dependent pathway. Compared to lenalidomide and pomalidomide, MGD-28 achieves deeper, faster, and more potent degradation of these neosubstrates. Additionally, MGD-28 exhibits broad antiproliferative activity in multiple solid malignancies and shows preferential cytotoxicity toward multiple myeloma patient-derived cells at various disease stages.
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名称 | MGD-28 |
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Iupac 化学名称 | 4-(4-(4-(((2-(2,6-dioxopiperidin-3-yl)-3-methyl-1-oxo-1,2,3,4-tetrahydrophthalazin-5-yl)amino)methyl)benzyl)piperazin-1-yl)-2-fluorobenzonitrile |
同义词 | MGD-28; MGD 28; MGD28; |
英文同义词 | MGD-28; MGD 28; MGD28; |
分子式 | C33H34FN7O3 |
分子量 | 595.67 |
Smile | CN(N(C1C(NC(CC1)=O)=O)C2=O)CC(C2=CC=C3)=C3NCC(C=C4)=CC=C4CN(CC5)CCN5C6=CC(F)=C(C#N)C=C6 |
InChiKey | JICHBFQDRLGJTM-UHFFFAOYSA-N |
InChi | InChI=1S/C33H34FN7O3/c1-38-21-27-26(33(44)41(38)30-11-12-31(42)37-32(30)43)3-2-4-29(27)36-19-22-5-7-23(8-6-22)20-39-13-15-40(16-14-39)25-10-9-24(18-35)28(34)17-25/h2-10,17,30,36H,11-16,19-21H2,1H3,(H,37,42,43) |
Cas号 | 2991818-13-2 |
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 | 类白色固体 |
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纯度 | 98% Min. |
存储 | 0-4℃,可保存几天到几周;-20℃,可保存 几个月。 |
可溶性 | 溶于DMSO等有机溶剂 |
处理方式 | |
运输条件 | 可以在室温下进行运输。 |
海关编码 |
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Mechanism | |
Cell study | |
Animal study | |
Clinical study |
Li P, Hu X, Fan Z, Sun S, Ran Q, Wei T, Wei P, Jiang Q, Yan J, Yang N, Jia C, Yang T, Mao Y, Cai X, Xu T, Zhao Z, Qian X, Qin W, Zhuang X, Fan F, Xiao J, Zheng Z, Li S. Novel potent molecular glue degraders against broad range of hematological cancer cell lines via multiple neosubstrates degradation. J Hematol Oncol. 2024 Sep 2;17(1):77. doi: 10.1186/s13045-024-01592-z. PMID: 39218923; PMCID: PMC11367868.