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ROC-325

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Chemical Structure| 1859141-26-6 同义名 : -
CAS号 : 1859141-26-6
货号 : A461073
分子式 : C28H27ClN4OS
纯度 : 99%+
分子量 : 503.058
MDL号 : MFCD31619252
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 4 mg/mL(7.95 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Autophagy
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.99mL

0.40mL

0.20mL

9.94mL

1.99mL

0.99mL

19.88mL

3.98mL

1.99mL
参考文献

[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.