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

ROC-325 

目录号: HY-103706 纯度: 99.91%
产品使用指南

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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10 mM * 1 mL in DMSO ¥1217
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100 mg ¥9900
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  • 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 antagonizes renal cell carcinoma (RCC) growth and survival in an ATG5/7-dependent manner, induces apoptosis, and exhibits favorable selectivity. ROC-325 inhibits cells growth with IC50 values of 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 and 6.0 μM for A498, A549, CFPAC-1, COLO-205, DLD-1, IGROV-1, MCF-7, MiaPaCa-2, NCI-H69, PC-3, RL and UACC-62 cells, respectively. ROC-325 induces hallmark features of autophagy inhibition and antagonizes autophagic flux[1].
ROC-325 triggers a highly significant increase in cathepsin D (CTSD) levels. Treatment with 5 μM ROC-325 for 24 hours leads to the formation of LC3B punctae and a robust increase in LC3B levels in both A498 and 786-0 RCC cells. Immunoblotting analysis conducted in both A498 and 786-0 cells demonstrates that ROC-325 promotes a dose-dependent increase in LC3B expression in a manner that correlated with a corresponding increase in the levels of p62 and cathepsin D[1].

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

体内研究
(In Vivo)

Oral administration of ROC-325 (25 mg/kg, 40 mg/kg, 50 mg/kg,) to mice bearing 786-0 RCC xenografts is well tolerated, significantly more effective at inhibiting tumor progression than Hydroxychloroquine, and inhibits autophagy in vivo[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
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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 32 mg/mL (63.61 mM; Need ultrasonic)

H2O : 1 mg/mL (1.99 mM; Need ultrasonic)

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
10 mM 0.1988 mL 0.9939 mL 1.9878 mL
*

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, 6 months; -20°C, 1 month。-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。

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
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  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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产品名称:
ROC-325
目录号:
HY-103706
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