ROC-325

Catalog No.S8527

ROC-325 Chemical Structure

Molecular Weight(MW): 503.06

ROC-325 is an orally available novel inhibitor of lysosomal-mediated autophagy which diminishes AML cell viability with the IC50 range of 0.7-2.2 μM.

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Biological Activity

Description ROC-325 is an orally available novel inhibitor of lysosomal-mediated autophagy which diminishes AML cell viability with the IC50 range of 0.7-2.2 μM.
Targets
Autophagy [1]
()
In vitro

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[1].

In vivo ROC-325 is well tolerated and no notable toxicities are observed other than a modest, non-significant reversible reduction in mean body weight[1]. 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[2].

Protocol

Solubility (25°C)

In vitro DMSO 4 mg/mL (7.95 mM)
Ethanol 4 mg/mL (7.95 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 503.06
Formula

C28H27ClN4OS

CAS No. 1859141-26-6
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Autophagy Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID