ROC-325 is an autophagy inhibitor. ROC-325 exhibited superior in vitro anticancer effects compared with the existing autophagy inhibitor hydroxychloroquine (HCQ) in 12 different cancer cell lines with diverse genetic backgrounds. ROC-325 antagonized RCC growth and survival in an ATG5/7-dependent manner, induced apoptosis, and exhibited favorable selectivity.
Chemical Formula: C28H27ClN4OS
Exact Mass: 502.1594
Molecular Weight: 503.061
Elemental Analysis: C, 66.85; H, 5.41; Cl, 7.05; N, 11.14; O, 3.18; S, 6.37
InChi Code: InChI=1S/C28H27ClN4OS/c1-18-7-10-23(26-27(34)21-5-3-4-6-25(21)35-28(18)26)32-14-16-33(2)15-13-31-22-11-12-30-24-17-19(29)8-9-20(22)24/h3-12,17,32H,13-16H2,1-2H3,(H,30,31)
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
ROC-325 antagonizes renal cell carcinoma (RCC) growth and survival in an ATG5/7-dependent manner, induces apoptosis, and exhibits favorable selectivity. ROC-325 inhibits cells growth with IC50 values of 4.9 μM, 11 μM, 4.6 μM, 5.4 μM, 7.4 μM, 11 μM, 8.2 μM, 5.8 μM, 5.0 μM, 11 μM, 8.4 μM and 6.0 μM for A498, A549, CFPAC-1, COLO-205, DLD-1, IGROV-1, MCF-7, MiaPaCa-2, NCI-H69, PC-3, RL and UACC-62 cells, respectively.
ROC-325 induces hallmark features of autophagy inhibition and antagonizes autophagic flux.
ROC-325 triggers a highly significant increase in cathepsin D (CTSD) levels. Treatment with 5 μM ROC-325 for 24 hours leads to the formation of LC3B punctae and a robust increase in LC3B levels in both A498 and 786-0 RCC cells. Immunoblotting analysis conducted in both A498 and 786-0 cells demonstrates that ROC-325 promotes a dose-dependent increase in LC3B expression in a manner that correlated with a corresponding increase in the levels of p62 and cathepsin D.
Oral administration of ROC-325 (25 mg/kg, 40 mg/kg, 50 mg/kg,) to mice bearing 786-0 RCC xenografts is well tolerated, significantly more effective at inhibiting tumor progression than Hydroxychloroquine, and inhibits autophagy in vivo.
Carew JS, Nawrocki ST. Drain the lysosome: Development of the novel orally available autophagy inhibitor ROC-325. Autophagy. 2017 Apr 3;13(4):765-766. doi: 10.1080/15548627.2017.1280222. Epub 2017 Jan 24. PubMed PMID: 28118053.
Carew JS, Espitia CM, Zhao W, Han Y, Visconte V, Phillips J, Nawrocki ST. Disruption of Autophagic Degradation with ROC-325 Antagonizes Renal Cell Carcinoma Pathogenesis. Clin Cancer Res. 2016 Nov 23. doi: 10.1158/1078-0432.CCR-16-1742. [Epub ahead of print] PubMed PMID: 27881580.
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