| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| A420319-1ml |
1ml |
现货  |
|
| 英文别名 | 2,6-Piperidinedione, 3-(5-amino-2-methyl-4-oxo-3(4H)-quinazolinyl)- | BDBM76986 | SCHEMBL282749 | 5,8-Dihydro-5,8-dioxo-6-(phenylamino)quinoline | CCG-267340 | MFCD29919294 | 28DZS29F59 | CC-122Avadomide | Emmatos | BP-27973 | GTPL10522 | BCP15938 | MAFEN |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Avadomide (CC-122) |
| 生化机理 | 阿伐多米（CC-122）是一种新的化学实体，被称为多生物通路调节剂，是治疗弥漫大 B 细胞淋巴瘤（DLBCL）的新型药物，具有抗肿瘤和免疫调节活性。它的分子靶点是脑龙蛋白（CRBN），脑龙蛋白是Cullin环E3泛素连接酶复合物CRL4CRBN的底物受体。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用机制 | 大脑 |
| 产品介绍 |
Avadomide (CC-122)，一种新型的多效性修饰剂化合物，在弥漫性大B细胞淋巴瘤（DLBCL）中具有抗肿瘤、免疫调节活性。其分子靶标为cereblon (CRBN)，CRBN是E3泛素化连接酶复合体CRL4CRBN的底物受体。 Information Avadomide (CC-122) Avadomide (CC-122), a new chemical entity termed pleiotropic pathway modifier, is a novel agent for Diffuse large B-cell lymphoma(DLBCL) with antitumor and immunomodulatory activity. Its molecular target is the protein cereblon (CRBN), a substrate receptor of the cullin ring E3 ubiquitin ligase complex CRL4 CRBN . Targets CRBN In vitro CC-122 is a novel agent for DLBCL with antitumor and immunomodulatory activity. In DLBCL cell lines, It binds CRBN and induces degradation or short hairpin RNA-mediated knockdown of Aiolos and Ikaros which correlates with increased transcription of interferon (IFN)-stimulated genes independent of IFN-α, -β, and -γ production and/or secretion and results in apoptosis in both activated B-cell (ABC) and germinal center B-cell DLBCL cell lines. CRBN is the molecular target of CC-122, CC-122 binding to CRBN recruits Aiolos/Ikaros to CRL4CRBN, and E3 ligase enzymatic activity is necessary for ubiquitination of Aiolos and Ikaros and thus their proteasomal degradation induced by CC-122. CC-122 induces IFN-regulated proteins and its mediated effects on the IFN pathway is independent of autocrine type I and II IFN secretion and signaling. In vivo CC-122 reduces tumor growth in xenograft models established from ABC- and GCB-DLBCL cell lines, and stimulates IL-2 production in primary T cells. Also, in a single-arm CC-122 clinical trial, exposure to CC-122 reduced expression levels of Aiolos and Ikaros in each patient by 25% to 50% demonstrating the utility of these 2 proteins as pharmacodynamic markers of CC-122. Cell Research(from reference) Cell lines：DLBCL cell lines(TMD8, U2932, Riva, and OCI-LY10) and GCB-DLBCL lines (Karpas 422, WSU-DLCL2, SUDHL-4, OCI-LY19, and Pfeiffer) Concentrations：0.01 to 10\u2009000 nM Incubation Time：5 days |
| ALogP | -0.477 |
|---|---|
| hba_count | 4 |
| HBD Count | 2 |
| Rotatable Bond | 1 |
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
| 分子类型 | 小分子 |
|---|---|
| IIUPAC Name | 3-(5-amino-2-methyl-4-oxoquinazolin-3-yl)piperidine-2,6-dione |
| INCHI | 1S/C14H14N4O3/c1-7-16-9-4-2-3-8(15)12(9)14(21)18(7)10-5-6-11(19)17-13(10)20/h2-4,10H,5-6,15H2,1H3,(H,17,19,20) |
| InChi Key | RSNPAKAFCAAMBH-UHFFFAOYSA-N |
| Smiles | CC1=NC2=CC=CC(=C2C(=O)N1C3CCC(=O)NC3=O)N |
| Isomeric SMILES | CC1=NC2=CC=CC(=C2C(=O)N1C3CCC(=O)NC3=O)N |
| 分子量 | 286.29 |
| Reaxy-Rn | 13123447 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=13123447&ln= |
| DMSO(mg / mL) Max Solubility | 57 |
|---|---|
| DMSO(mM) Max Solubility | 199.0988159 |
| Water(mg / mL) Max Solubility | ＜1 |
| 分子量 | 286.290 g/mol |
| XLogP3 | 0.000 |
| 氢键供体数Hydrogen Bond Donor Count | 2 |
| 氢键受体数Hydrogen Bond Acceptor Count | 5 |
| 可旋转键计数Rotatable Bond Count | 1 |
| 精确质量Exact Mass | 286.107 Da |
| 单同位素质量Monoisotopic Mass | 286.107 Da |
| 拓扑极表面积Topological Polar Surface Area | 105.000 Ų |
| 重原子数Heavy Atom Count | 21 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 530.000 |
| 同位素原子数Isotope Atom Count | 0 |
| 定义的原子立体中心计数Defined Atom Stereocenter Count | 0 |
| 未定义的原子立体中心计数Undefined Atom Stereocenter Count | 1 |
| 定义的键立体中心计数Defined Bond Stereocenter Count | 0 |
| 未定义的键立体中心计数Undefined Bond Stereocenter Count | 0 |
| 所有立体化学键的总数The total count of all stereochemical bonds | 0 |
| 共价键合单元计数Covalently-Bonded Unit Count | 1 |
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