ROC-325|cas:1859141-26-6|西域试剂

ROC-325,99.91%

产品编号：Bellancom-103706| CAS NO：1859141-26-6| 分子式：C₂₈H₂₇ClN₄OS| 分子量：503.06

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货号	价格	库存与货期
Bellancom-103706	￥1100.00	杭州北京（现货）
Bellancom-103706	￥1700.00	杭州北京（现货）
Bellancom-103706	￥3400.00	杭州北京（现货）
Bellancom-103706	￥5500.00	杭州北京（现货）
Bellancom-103706	￥9900.00	杭州北京（现货）

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ROC-325

产品介绍

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)。

生物活性

ROC-325 is a potent and orally active autophagy inhibitor with a strong anticancer activity. ROC-325 induces the deacidification of lysosomes, accumulation of autophagosomes, and disrupted autophagic flux. ROC-325 also induces renal cell carcinoma apoptosis.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : 32 mg/mL (63.61 mM; Need ultrasonic)

H₂O : 1 mg/mL (1.99 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9878 mL	9.9392 mL	19.8783 mL
5 mM	0.3976 mL	1.9878 mL	3.9757 mL
10 mM	0.1988 mL	0.9939 mL	1.9878 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式