|1-((2-((2-((7-氯喹啉-4-基)氨基)乙基)(甲基)氨基)乙基)氨基)-4-甲基-9H-硫杂蒽-9-酮|CsnPharm

CAS No.: 1859141-26-6

ROC-325 Catalog No. CSN20231

Synonyms: ROC-325

ROC-325 is an inhibitor of autophagy with promising anti-leukemic activity, which diminishes AML cell viability with the IC50 range of 0.7-2.2 μM.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Autophagy is an evolutionarily conserved mechanism of lysosomal proteolysis that is used for the turnover of organelles and proteins with long half-lives and also functions to generate alternative sources of metabolic fuel via nutrient recycling under stress conditions^[3]. ROC-325 is a novel inhibitor of autophagy. Treatment with ROC-325 results in a significant loss of acridine orange fluorescence. ROC-325 triggers a highly significant increase in cathepsin D (CTSD) levels. ROC-325 treatment yields pharmacodynamic effects that are consistent with inhibition of autophagy. 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^[3]. ROC-325 is well tolerated and no notable toxicities are observed other than a very modest, nonsignificant reduction in mean body weight at the highest dose. Immunohistochemical analysis of specimens collected from animals treated with ROC-325 demonstrates significant, dose-dependent increases in the autophagic markers LC3B and p62 and increases apoptosis^[3].
动物研究
剂量
Mice: 25 mg/kg - 50 mg/kg^[1] (p.o.)

给药途径
p.o.
参考文献

动物研究
剂量	Mice: 25 mg/kg - 50 mg/kg^[1] (p.o.)
给药途径	p.o.

[1] Carew JS, Espitia CM, et al. Disruption of Autophagic Degradation with ROC-325 Antagonizes Renal Cell Carcinoma Pathogenesis. Clin Cancer Res. 2017 Jun 1;23(11):2869-2879.
[2] Carew JS, Nawrocki ST. Drain the lysosome: Development of the novel orally available autophagy inhibitor ROC-325. Autophagy. 2017 Apr 3;13(4):765-766.
[3] Carew JS, Espitia CM, Zhao W, Han Y, Visconte V, Phillips J, Nawrocki ST. Disruption of Autophagic Degradation with ROC-325 Antagonizes Renal Cell Carcinoma Pathogenesis. Clin Cancer Res. 2017 Jun 1;23(11):2869-2879. doi: 10.1158/1078-0432.CCR-16-1742. Epub 2016 Nov 23. PMID: 27881580; PMCID: PMC5593077.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9878 mL
- 9.9392 mL
- 19.8784 mL
- 5 mM
- 0.3976 mL
- 1.9878 mL
- 3.9757 mL
- 10 mM
- 0.1988 mL
- 0.9939 mL
- 1.9878 mL

技术信息

CAS号

1859141-26-6

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H27ClN4OS

运输

蓝冰

分子量

503.06

别名

ROC-325

溶解度

DMSO	44.0 mg/mL (87.5 mM)
Water	insoluble

动物实验配方

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ROC-325 Catalog No. CSN20231

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