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.

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Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

ROC325；ROC 325

powder

DMSO : 32 mg/mL (63.61 mM)

Autophagy

Treatment with ROC-325 triggers all of the hallmark features of autophagy inhibition including the accumulation of autophagosomes with undegraded cargo, an increase in lysosomal membrane permeability, deacidification of lysosomes, and elevated LC3B, p62, and cathepsin D expression. In vitro treatment of a panel of human AML cell lines and normal human bone marrow progenitors demonstrate that ROC-325 diminishes AML cell viability (IC50 range 0.7-2.2 µM), antagonizes clonogenic survival, and induces apoptosis in a manner that is therapeutically selective.

ROC-325 is well tolerated and no notable toxicities are observed other than a modest, non-significant reversible reduction in mean body weight. Oral administration of ROC-325 to mice bearing RCC xenografts is well tolerated and yields dose-dependent inhibition of tumor growth that is significantly more efficacious than a higher dose of HCQ.