规格

价格

库存

数量

1 mg

¥ 361

现货

2 mg

¥ 528

现货

5 mg

¥ 913

现货

10 mg

¥ 1,390

现货

25 mg

¥ 3,160

现货

50 mg

¥ 4,630

现货

100 mg

¥ 6,620

现货

500 mg

¥ 13,300

待询

1 mL x 10 mM (in DMSO)

¥ 973

现货

生物活性

产品描述	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.
靶点活性	p97 AAA ATPase:11 nM
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]
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.
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)
别名	CB5083, CB 5083

化学信息

分子量	413.47
分子式	C₂₄H₂₃N₅O₂
CAS No.	1542705-92-9
Smiles	Cc1cc2c(cccc2n1-c1nc2CCOCc2c(NCc2ccccc2)n1)C(N)=O
密度	1.37 g/cm3 (Predicted)

储存&溶解度

存储

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.

实际储存温度请以COA为准

溶解度信息

Ethanol: 11 mg/mL (26.6 mM), Sonication is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 247.5 mg/mL (598.59 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 6 mg/mL (14.51 mM), Solution.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4186 mL	12.0928 mL	24.1856 mL	120.9278 mL
5 mM	0.4837 mL	2.4186 mL	4.8371 mL	24.1856 mL
10 mM	0.2419 mL	1.2093 mL	2.4186 mL	12.0928 mL
20 mM	0.1209 mL	0.6046 mL	1.2093 mL	6.0464 mL

DMSO

	1mg	5mg	10mg	50mg
50 mM	0.0484 mL	0.2419 mL	0.4837 mL	2.4186 mL
100 mM	0.0242 mL	0.1209 mL	0.2419 mL	1.2093 mL

该溶液配制表仅适用于固体产品。对于液体产品，请根据标明的浓度或密度计算稀释方案。

CB-5083

CB-5083

产品介绍

引用文献

计算器

体内实验配液计算器

剂量转换

关键词

CB-5083

CB-5083

CB-5083 相关产品

产品介绍

引用文献

计算器

体内实验配液计算器

剂量转换

关键词