All AbMole products are for research use only, cannot be used for human consumption.
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.
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. 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.
| Cell Experiment | |
|---|---|
| Cell lines | RCC cells |
| Preparation method | RCC cells were treated with ROC-325 for 24 h and harvested for imaging. Briefly, sections were cut in an LKB Ultracut microtome (Leica), stained with uranyl acetate and lead citrate, and examined in a JEM 1230 transmission electron microscope. |
| Concentrations | 1 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Mice |
| Formulation | water |
| Dosages | 25, 40, and 50 mg/kg |
| Administration | p.o. |
| Molecular Weight | 503.06 |
| Formula | C28H27ClN4OS |
| CAS Number | 1859141-26-6 |
| Solubility (25°C) | 4 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Autophagy Products |
|---|
| Vacuolin-1
Vacuolin-1 is a cell-permeable inhibitor of Ca2+ dependent fusion of lysosomes to the cell membrane. Vacuolin-1 blocks the Ca2+-dependent exocytosis of lysosomes and prevents the release of lysosomal content without affecting the process of resealing. vacuolin‐1 is a potent and selective PIKfyve inhibitor and inhibits late‐stage autophagy by impairing lysosomal maturation. |
| CA77.1
CA77.1 is a potent, brain-penetrant and orally active chaperone-mediated autophagy (CMA) activator with favorable pharmacokinetics. |
| KAN0438757
KAN0438757 is a potent and selective inhibitor of the metabolic kinase PFKFB3 with an IC50 of 0.19 μM. |
| Metofenazate
Metofenazate is a selective calmodulin inhibitor. |
| Patulin
Patulin (Terinin) is a mycotoxin produced by a variety of fungi, causes chromosome breakage, mutation, teratogenic and cytotoxic. Patulin induces autophagy-dependent apoptosis through lysosomal-mitochondrial axis, and causes DNA damage. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
