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- 2026年07月07日
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- CAS号：
1542705-92-9
- 规格：
1mLx10mM(inDMSO)/1mg/2mg/5mg/10mg/25mg/50mg/100mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥778.0 |
|---|---|---|---|
| 规格： | 1mg | 产品价格： | ￥304.0 |
| 规格： | 2mg | 产品价格： | ￥422.0 |
| 规格： | 5mg | 产品价格： | ￥730.0 |
| 规格： | 10mg | 产品价格： | ￥1112.0 |
| 规格： | 25mg | 产品价格： | ￥2528.0 |
| 规格： | 50mg | 产品价格： | ￥3704.0 |
| 规格： | 100mg | 产品价格： | ￥5296.0 |
Product Introduction
Bioactivity
| 名称 | CB-5083 |
| 描述 | CB-5083 is an effective, selective, orally available p97 AAA ATPase inhibitor with an IC50 of 11 nM. CB-5083 exhibits broad-spectrum antitumor activity. CB-5083 can be used in studies of protein homeostasis disruption, endoplasmic reticulum stress, and tumor drug resistance. |
| 细胞实验 | A549 and other tumor cell lines are cultured according to ATCC guidelines. Cells are cultured in black or white, clear-bottomed, tissue culture-treated 384-well plates. Cells are treated with 10-point dose titration of the compound in well duplicates. After a 72 h treatment, CellTiter-Glo is added to the white plates to measure cell viability. Luminescence values are fit to a four-parameter sigmoidal curve to determine IC50 concentrations.(Only for Reference) |
| 激酶实验 | ATPase assay: Compounds are diluted in DMSO with a 3-fold 10-point serial dilution starting at 10 μM. The assay is done in a 384-well plate with each row as a single dilution series with duplicate of each compound concentration point. In 5 μL total volume, 20 nM p97 hexameric enzyme and 20 μM ATP are added to start the reaction. The plate is sealed and incubated at 37 °C for 15 min after mixing thoroughly in an orbital shaker. Compound dilution, ATP and enzymes addition are conducted with automated liquid handling using the Freedom Evo. ADP Glo reagents 1 and 2 are added according to the manufacturer's protocol. The luminescence is measured by Envision plate reader as the end point of the reaction. The IC50 of each compound is derived by fitting the luminescence values to a four-parameter sigmoidal curve. |
| 体外活性 | 方法：患者来源成肌细胞（p.R155H），加入 CB-5083 （75， 100， 150 nM），处理 5 天，Western blot 检测 MFN2， p62， LC3， TFEB， VCP 蛋白水平。 结果：CB-5083 诱导 MFN2 水平显著上调，自噬标志物 p62 和 LC3-II/I 比值显著增加，TFEB 和总 VCP 水平无显著变化。[1] 方法：11 种骨肉瘤细胞系（U2OS， HOS， SJSA-1 等）及人成骨细胞 hFOB1.19，加入浓度梯度 CB-5083 （0–8 μM） ，处理 72 小时，MTT 法检测细胞活力，计算半数抑制浓度（IC₅₀）。 结果：CB-5083 对骨肉瘤细胞的 IC₅₀范围为 0.3286–1.032 μM，呈剂量依赖性抑制。[2] |
| 体内活性 | 方法：VCPR 155H/R155H 纯合小鼠(2 月龄)，口服灌胃 CB-5083，15 mg/kg/天，每日一次，持续 5 个月。 结果：CB-5083 耐受良好，体重正常，血清 AST 和 CK 有降低趋势，无肝毒性，Rotarod 表现无显著恶化。[1] 方法：裸鼠，皮下接种 SJSA-1 细胞，待肿瘤体积达 100 mm³后开始口服灌胃给药 CB-5083 (100 mg/kg/天)，每日一次，持续 30 天。 结果：CB-5083 治疗组从第 15 天起肿瘤体积显著小于对照组，终点平均肿瘤重量对照组 823 mg 显著高于 CB-5083 组 416 mg。[2] |
| 存储条件 | Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | Ethanol : 11 mg/mL (26.6 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 6 mg/mL (14.51 mM), Solution. H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 247.5 mg/mL (598.59 mM), Sonication is recommended. |
| 关键字 | VCP | tumors | solid | p97 | myeloma | multiple | Inhibitor | inhibit | Cdc48 | CB-5083 | ATPase | AAA |
| 相关产品 | MNS | VCP/p97 inhibitor-1 | MSC1094308 | NMS-859 | ML241 hydrochloride | NMS-873 | NPD8733 | Eeyarestatin I | NSC819701 | CB-5339 | DBEQ | ML240 |
| 相关库 | Inhibitor Library | Bioactive Compound Library | Anti-Cancer Active Compound Library | Bioactive Compounds Library Max | Failed Clinical Trials Compound Library | NO PAINS Compound Library | Anti-Viral Compound Library | Orally Active Compound Library | Drug Repurposing Compound Library | Anti-Cancer Clinical Compound Library | Target-Focused Phenotypic Screening Library | Anti-Cancer Drug Library |
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化合物 CB5083【1542705-92-9】
￥304 - 5296
