ROC-325
目录号 : GC32901
An autophagy inhibitor
Cas No.:1859141-26-6
Sample solution is provided at 25 µL, 10mM.
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ROC-325 is an autophagy inhibitor.1 It inhibits autophagic flux and induces lysosomal deacidification and apoptosis in 786-O renal cell carcinoma cells when used at a concentration of 5 ?M. ROC-325 decreases viability in a panel of 12 cancer cell lines, including renal, lung, pancreatic, and prostate cancer cells, with IC50 values ranging from 4.9 to 11 ?M. It reduces tumor growth in a 786-O mouse xenograft model when administered at a dose of 50 mg/kg. ROC-325 also decreases the cytopathic effect of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in infected Vero E6 cells (EC50 = 3.28 ?M).2
1.Carew, J.S., Espitia, C.M., Zhao, W., et al.Disruption of autophagic degradation with ROC-325 antagonizes renal cell carcinoma pathogenesisClin. Cancer Res.23(11)2869-2879(2017) 2.Gorshkov, K., Chen, C.Z., Bostwick, R., et al.The SARS-CoV-2 cytopathic effect is blocked by lysosome alkalizing small moleculesACS Infect. Dis.(2020)
Kinase experiment: | Renal cancer cells are incubated with ROC-325 for 24 hours. Cells are harvested and then lysed. Approximately 50 μg of total cellular protein from each sample are subjected to SDS-PAGE, proteins are transferred to nitrocellulose membranes, and the membranes are blocked with 5% nonfat milk in a Tris-buffered saline solution containing 0.1% Tween-20 for 1 hour. The blots are then probed overnight at 4°C with primary antibodies, washed, and probed with species-specific secondary antibodies coupled to horseradish peroxidase. Immunoreactive material is detected by enhanced chemiluminescence[1]. |
Cell experiment: | Cell viability is estimated by the MTT assay. Cells are seeded into 96-well microcultureplates at 10,000 cells per well and allowed to attach for 24 hours. Cells are then treated with ROC-325 for 72 hours. Following ROC-325 treatment, MTT is added and formazan absorbance is quantified using a microplate reader. The estimated cell viability under each experimental condition is calculated by normalizing the respective formazan optical density to the density of control cells. Proapoptotic effects following in vitro ROC-325 exposure are quantified by propidium iodide (PI) staining and fluorescence-activated cell sorting (FACS) analysis of sub-G0/G1 DNA content and by measurement of active caspase-3 by flow cytometry using a commercial kit[1]. |
Animal experiment: | 786-0 renal cancer cells (5×106) are suspended in a mixture of HBSS and Matrigel and subcutaneously implanted into female nude mice. Tumor-bearing animals from each cell line xenograft are randomized into treatment groups. Mice are treated with vehicle (water), ROC-325 (25, 40, and 50 mg/kg PO) QD×5 for 6 weeks. Mice are monitored daily and tumor volumes are measured twice weekly. At study completion, tumors from representative animals are excised from each group, formalin-fixed, and paraffin-embedded for immunohistochemical analysis[1]. |
References: [1]. Carew JS, et al. Disruption of Autophagic Degradation with ROC-325 Antagonizes Renal Cell Carcinoma Pathogenesis. Clin Cancer Res. 2017 Jun 1;23(11):2869-2879. | |
| Cas No. | 1859141-26-6 | SDF | |
| Canonical SMILES | O=C1C2=C(SC3=C1C=CC=C3)C(C)=CC=C2NCCN(CCNC4=CC=NC5=CC(Cl)=CC=C45)C | ||
| 分子式 | C28H27ClN4OS | 分子量 | 503.06 |
| 溶解度 | DMSO : 32 mg/mL (63.61 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9878 mL | 9.9392 mL | 19.8783 mL |
| 5 mM | 0.3976 mL | 1.9878 mL | 3.9757 mL |
| 10 mM | 0.1988 mL | 0.9939 mL | 1.9878 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet