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ROC-325

Cat. No. M6260
ROC-325 Structure
Size Price Availability
10mg USD 210 1-2 Weeks
25mg USD 425 1-2 Weeks
50mg USD 680 1-2 Weeks
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Protocol
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 503.06
Formula C28H27ClN4OS
CAS Number 1859141-26-6
Purity >98%
Solubility 4 mg/mL in DMSO
Storage at -20°C
References

Drain the lysosome: Development of the novel orally available autophagy inhibitor ROC-325.
Carew JS, et al. Autophagy. 2017 Apr 3;13(4):765-766. PMID: 28118053.

Disruption of Autophagic Degradation with ROC-325 Antagonizes Renal Cell Carcinoma Pathogenesis.
Carew JS, et al. Clin Cancer Res. 2017 Jun 1;23(11):2869-2879. PMID: 27881580.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: ROC-325 supplier, Autophagy, inhibitors

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