1. Autophagy Apoptosis
  2. Autophagy Apoptosis
  3. ROC-325

ROC-325 是一种有效的具有口服活性的自噬 (autophagy) 抑制剂,具有很强的抗癌活性。ROC-325 引起溶酶体脱酸,自噬体积累和自噬通量中断。ROC-325 还诱导肾细胞癌凋亡 (apoptosis)。

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ROC-325 Chemical Structure

ROC-325 Chemical Structure

CAS No. : 1859141-26-6

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1217
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1 mg ¥502
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5 mg ¥1053
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10 mg ¥1638
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25 mg ¥3275
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50 mg ¥4863
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100 mg ¥6975
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200 mg   询价  
500 mg   询价  

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Customer Review

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

ROC-325 is a potent and orally active autophagy inhibitor with a strong anticancer activity. ROC-325 induces the deacidification of lysosomes, accumulation of autophagosomes, and disrupted autophagic flux. ROC-325 also induces renal cell carcinoma apoptosis[1].

IC50 & Target

Autophagy[1]

体外研究
(In Vitro)

ROC-325 以 ATG5/7 依赖性方式拮抗肾细胞癌 (RCC) 的生长和存活,诱导细胞凋亡,并表现出良好的选择性。ROC-325 抑制 A498、A549、CFPAC-1、COLO -205、DLD-1、IGROV-1、MCF-7、MiaPaCa-2、NCI-H69、PC-3、RL 和 UACC-62 细胞生长,IC50 值分别为 4.9 μM、11 μM、4.6 μM、5.4 μM、7.4 μM、11 μM、8.2 μM、5.8 μM、5.0 μM、11 μM、8.4 μM和 6.0 μM。ROC-325 诱导自噬抑制的标志性特征并拮抗自噬通量[1]
ROC-325 引发组织蛋白酶 D (CTSD) 水平的显著增加。用 5 μM ROC-325 处理 24 小时导致 LC3B 斑点的形成和 A498 和 786-0 RCC 细胞中 LC3B 水平的强劲增加。在 A498 和 786-0 细胞中进行的免疫印迹分析表明,ROC-325 促进 LC3B 表达的剂量依赖性增加,其方式与 p62 和组织蛋白酶 D 水平的相应增加相关[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

对携带 786-0 RCC 异种移植物的小鼠口服 ROC-325 (25 mg/kg、40 mg/kg、50 mg/kg) 具有良好的耐受性,在抑制肿瘤进展方面比羟氯喹更有效,并抑制体内自噬[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

503.06

Formula

C28H27ClN4OS

CAS 号
性状

固体

颜色

Light yellow to orange

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
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 4.55 mg/mL (9.04 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.61%

参考文献
Kinase Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

ROC-325 相关分类

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9878 mL 9.9392 mL 19.8783 mL 49.6959 mL
5 mM 0.3976 mL 1.9878 mL 3.9757 mL 9.9392 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
ROC-325
目录号:
HY-103706
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