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 |
|---|
| Tacrolimus (FK506)
Tacrolimus (FK506, FR900506, Fujimycin, Prograf) is a potent, clinically-useful immunosuppressant in the same molecular class as cyclosporin A and rapamycin. *The compound is unstable in solutions, freshly prepared is recommended |
| Metformin hydrochloride
Metformin HCl is a biguanide inhibitor that reduces blood glucose mainly by inhibiting hepatic glycogen production (hepatic gluconeogenesis), while Metformin is a CD47 inhibitor in vitro. |
| Ginkgolide K
Ginkgolide K induces protective autophagy through the AMPK/mTOR/ULK1 signaling pathway. |
| Ivermectin (MK-933)
Ivermectin (MK-933) is a positive allosteric modulator of the α7 neuronal nicotinic acetylcholine receptor and the purinergic P2X4 receptor. Importin α5 inhibitor ivermectin effectively abrogates STAT1-importin α5 interactions. |
| Bergapten
Bergapten is a psoralen that can be photoactivated and is capable of crossing-linking DNA, covalently modifying proteins and lipids, and consequently inhibiting cell replication. |
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 2010-2026 AbMole BioScience. All Rights Reserved.
