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Avadomide

E3 连接酶抑制剂
规格或纯度: 99%
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cereblon
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基本描述

别名 3-(5-氨基-2-甲基-4-氧代喹唑啉-3(4H)-基)-哌啶-2,6-二酮
规格或纯度 99%
英文名称 Avadomide
生化机理 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 CRL4CRBN.
储存温度 -20°C储存
运输条件 超低温冰袋运输
产品介绍

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?

产品属性

ALogP -0.477
HBD Count 2
Rotatable Bond 1

名称和标识符

IUPAC Name 3-(5-amino-2-methyl-4-oxoquinazolin-3-yl)piperidine-2,6-dione
INCHI 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
Canonical SMILES CC1=NC2=CC=CC(=C2C(=O)N1C3CCC(=O)NC3=O)N
PubChem CID 24967599
分子量 286.29

化学和物理性质

溶解性 Solubility (25°C) In vitro DMSO: 57 mg/mL (199.09 mM); Water: Insoluble; Ethanol: Insoluble;
DMSO(mg / mL) Max Solubility 57
DMSO(mM) Max Solubility 199.0988159
Water(mg / mL) Max Solubility ＜1

关联配体

Ligand ID 10522
名称 avadomide
别名 CC-122
类别 Synthetic organic
学名 3-(5-amino-2-methyl-4-oxoquinazolin-3-yl)piperidine-2,6-dione
生物活性评价 Avadomide (CC-122) stimulates IL-2 production in primary T cells, and causes apoptosis of lymphoma cells via direct derepression of interferon-stimulated gene transcription .
评价 Avadomide (CC-122) is a cereblon (CRBN)-targeting compound that exhibits potent single-agent clinical antitumour and immunomodulatory activities . It retains the glutarimide moiety that is shared by all thalidomide family drugs, and which is known to directly interact with CRBN. The INN record specifies avadomide as a racemic mixture of enantiomers. We show the structure without specified stereochemistry to represent the mixture. It is claimed as Compound A in Celgene's patent WO2014039960A1 .
配体家族 PROTACs, molecular glues and other degraders

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附件产品

  1. 阿瓦多米德(CC-122)
    阿瓦多米德(CC-122), 10mM in DMSO, 1ml

    ￥969.90

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参考文献

1. Hagner PR, Man HW, Fontanillo C, Wang M, Couto S, Breider M, Bjorklund C, Havens CG, Lu G, Rychak E et al..  (2015)  CC-122, a pleiotropic pathway modifier, mimics an interferon response and has antitumor activity in DLBCL..  Blood,  126  (6):  (779-89).  [PMID:26002965]
2. Rasco DW, Papadopoulos KP, Pourdehnad M, Gandhi AK, Hagner PR, Li Y, Wei X, Chopra R, Hege K, DiMartino J et al..  (2019)  A First-in-Human Study of Novel Cereblon Modulator Avadomide (CC-122) in Advanced Malignancies..  Clin Cancer Res,  25  (1):  (90-98).  [PMID:30201761]
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