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- 保存条件:
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
1859141-26-6
- 规格:
1 mg/5 mg/10 mg/25 mg/50 mg
| 规格: | 1 mg | 产品价格: | ¥502.0 |
|---|---|---|---|
| 规格: | 5 mg | 产品价格: | ¥1053.0 |
| 规格: | 10 mg | 产品价格: | ¥1638.0 |
| 规格: | 25 mg | 产品价格: | ¥3275.0 |
| 规格: | 50 mg | 产品价格: | ¥4863.0 |
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ROC-325
CAS No. : 1859141-26-6
MCE 国际站:ROC-325
产品活性:ROC-325 是一种有效的具有口服活性的自噬 (autophagy) 抑制剂,具有很强的抗癌活性。ROC-325 引起溶酶体脱酸,自噬体积累和自噬通量中断。ROC-325 还诱导肾细胞癌凋亡 (apoptosis)。
In Vitro: 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.
In Vivo: 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.
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