ROC-325 是一种有效的口服活性自噬抑制剂，具有抗癌活性。 ROC-325 诱导肾细胞癌凋亡并表现出良好的特异性。

ROC-325 is an effective and orally active inhibitor of autophagy with anticancer activity. ROC-325 induces renal cell carcinoma apoptosis and exhibits favorable selectivity.

ROC-325 (5 μM) leads to the formation of LC3B punctae and a robust increase in LC3B levels in both A498 and 786-0 RCC cells. 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. 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 the deacidification of lysosomes, accumulation of autophagosomes, and disrupted autophagic flux[1].

In mice bearing 786-0 RCC xenografts, ROC-325 (25, 40, and 50 mg/kg; oral) leads to significant, dose-dependent inhibition of disease progression and inhibits autophagy in vivo[1].

1859141-26-6

C28H27ClN4OS

503.06

H2O:0.8 mg/mL (1.59 mM),Need ultrasonic
DMSO:30 mg/mL (59.64 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years