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Avadomide

(Synonyms: CC 122)

目录号: PL01086 纯度: ≥99%

Avadomide (CC 122) 是口服有效的 cereblon 调节剂。Avadomide 可以调节 cereblon E3 连接酶活性，诱导弥漫性大 B 细胞淋巴瘤 (DLBCL) 细胞凋亡 (apoptosis)。 Avadomide 具有抗肿瘤和免疫调节活性。

CAS No. :1015474-32-4

商品编号	规格	价格	会员价
PL01086-5mg	5mg	¥533.00	请登录
PL01086-10mg	10mg	¥823.00	请登录
PL01086-50mg	50mg	¥2585.00	请登录
PL01086-100mg	100mg	¥4125.00	请登录
PL01086-200mg	200mg	¥5875.00	请登录
PL01086-500mg	500mg	询价	询价
PL01086-1 mL x 10 mM (in DMSO)	1 mL x 10 mM (in DMSO)	¥584.00	请登录

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中文名称	Avadomide
中文别名	3-(5-氨基-2-甲基-4-氧喹唑啉-3(4H)-基)哌啶-2,6-二酮
英文名称	Avadomide
英文别名	CC122;CC-122;Avadomide(CC-122);3-(5-amino-2-methyl-4-oxoquinazolin-3(4H)-yl)piperidine-2,6-dione;3-(5-amino-2-methyl-4-oxo-4H-quinazolin-3-yl)piperidine-2,6-dione;Avadomide;CC 122;3-(5-amino-2-methyl-4-oxo-4H-quinazolin-3-yl)-piperidine-2,6-dione;2,6-Piperidinedione, 3-(5-amino-2-methyl-4-oxo-3(4H)-quinazolinyl)-;2,6-Piperidinedione, 3-(5-amino-2-methyl-4-oxo-3(4H)-quinazolinyl)-;Avadomide [USAN];Avadomide (USAN/INN);US9694015, Compound A;BDBM76986;RSNPAKAFCAAMBH-UHFFFAOYSA-N;BCP15938;s7892;SB18829;AK31
Cas No.	1015474-32-4
分子式	C₁₄H₁₄N₄O₃
分子量	286.29
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	Avadomide (CC 122) 是口服有效的 cereblon 调节剂。Avadomide 可以调节 cereblon E3 连接酶活性，诱导弥漫性大 B 细胞淋巴瘤 (DLBCL) 细胞凋亡 (apoptosis)。 Avadomide 具有抗肿瘤和免疫调节活性。

产品详情

生物活性

Avadomide (CC 122) is an orally active cereblon modulator. Avadomide modulates cereblon E3 ligase activity and induces apoptosis of diffuse large B-cell lymphoma (DLBCL) cell lines. Avadomide exhibits potent antitumor and immunomodulatory activities.

性状

Solid

体外研究(In Vitro)

Avadomide inhibits proliferation and induces apoptosis in ABC and GCB DLBCL. In DLBCL cell lines, Avadomide-induced degradation or short hairpin RNA-mediated knockdown of Aiolos and Ikaros correlates with increased transcription of 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.[1] has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Treatment of female CB-17 SCID mice with Avadomide (CC122) at 3 or 30 mg/kg once daily significantly decreased tumor growth in OCI-LY10 ABC-DLBCL (P = .028 and P < .001, respectively) and WSU-DLCL2 GCB-DLBCL derived xenograft models (P < .01) compared with the vehicle control. In a separate study, we assessed the ability of Avadomide (CC122) to promote degradation of Ikaros and Aiolos in vivo. In the 21-day efficacy study of WSU-DLCL2 xenograft transplanted mice, tumors were excised 1, 6, or 24 hours post final dosing. Aiolos and Ikaros expression was interrogated through immunohistochemistry (IHC) and was found to be decreased 64% and 30%, respectively, compared with vehicle within 1 hour of treatment, with a maximal reduction of 94% and 69%, respectively, observed at 6 hours. Aiolos and Ikaros levels partially recovered 24 hours postdosing with protein level within 20%

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Rasco DW, et al. A First-in-Human Study of Novel Cereblon Modulator Avadomide (CC-122) in Advanced Malignancies. Clin Cancer Res. 2019 Jan 1;25(1):90-98.
[2]. Hagner, P.R.et al.CC-122, a pleiotropic pathway modifier, mimics an IFN response and has antitumor activity in DLBCL.Blood.Aug 6;126(6):779-89.

溶解度数据	In Vitro: DMSO : 33.33 mg/mL (116.42 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Avadomide

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