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Formula | C28H27ClN4OS |
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Molecular Weight | 503.06 | CAS No. | 1859141-26-6 | |
Solubility (25°C)* | In vitro | DMSO | 4 mg/mL (7.95 mM) | |
Ethanol | 4 mg/mL (7.95 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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. | |
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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]. |
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Mitophagy regulates mitochondrial number following pharmacological induction of mitochondrial biogenesis in renal proximal tubule cells [ Front Pharmacol, 2024, 15:1344075] | PubMed: 38375036 |
Reserpine maintains photoreceptor survival in retinal ciliopathy by resolving proteostasis imbalance and ciliogenesis defects [ Elife, 2023, 12e83205] | PubMed: 36975211 |
ASCL2 Maintains Stemness Phenotype through ATG9B and Sensitizes Gliomas to Autophagy Inhibitor [ Adv Sci (Weinh), 2022, 9(27):e2105938] | PubMed: 35882624 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
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