Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Avadomide (CC 122) 是口服有效的cereblon 调节剂,可以调节 cereblon E3 连接酶活性,诱导弥漫性大 B 细胞淋巴瘤细胞凋亡,具有抗肿瘤和免疫调节活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 319 | 现货 | ||
2 mg | ¥ 453 | 现货 | ||
5 mg | ¥ 747 | 现货 | ||
10 mg | ¥ 1,230 | 现货 | ||
25 mg | ¥ 2,260 | 现货 | ||
50 mg | ¥ 3,730 | 现货 | ||
100 mg | ¥ 5,420 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 822 | 现货 |
产品描述 | Avadomide (CC 122) is an orally available pleiotropic pathway modulator with potential antineoplastic activity. |
体外活性 | 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[1]. |
体内活性 | 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 Clinicalal 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[1]. |
细胞实验 | Diffuse Large B-Cell Lymphoma are cultured in RPMI-1640 containing 10-20% fetal bovine serum, 1% Penicillin/Streptomycin and 1 mM sodium pyruvate. 2×104 cells are plated per well in media containing either DMSO or various concentrations of CC-122. Cells are cultured for 5 days at 37 degrees Celsius after which tritiated thymidine is added to the cell culture for the final 6 hours. Cells are subsequently harvested onto filter plates. After the plates have dried, scintillation fluid is added to the plates and read on a Top-count reader(Only for Reference) |
别名 | CC 122 |
分子量 | 286.29 |
分子式 | C14H14N4O3 |
CAS No. | 1015474-32-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 1 mg/mL (3.49 mM)
DMSO: 52 mg/mL(181.7 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 3.493 mL | 17.4648 mL | 34.9296 mL | 87.324 mL |
DMSO | 5 mM | 0.6986 mL | 3.493 mL | 6.9859 mL | 17.4648 mL |
10 mM | 0.3493 mL | 1.7465 mL | 3.493 mL | 8.7324 mL | |
20 mM | 0.1746 mL | 0.8732 mL | 1.7465 mL | 4.3662 mL | |
50 mM | 0.0699 mL | 0.3493 mL | 0.6986 mL | 1.7465 mL | |
100 mM | 0.0349 mL | 0.1746 mL | 0.3493 mL | 0.8732 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Avadomide 1015474-32-4 Apoptosis PROTAC Ubiquitination E1/E2/E3 Enzyme Ligand for E3 Ligase orally diffuse CC122 CC-122 B-cell Inhibitor DLBCL Ubiquitin ligase E3 ligating enzyme immunomodulatory cereblon E1 activating enzyme ligase E2 conjugating enzyme large CC 122 Ubiquitin conjugating enzyme Ubiquitin activating enzyme antitumor inhibit lymphoma inhibitor