RK-33

MCE 国际站：RK-33

CAS：1070773-09-9

品牌：MedChemExpress (MCE)

存储条件：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

生物活性：RK-33 是 RNA helicase 的抑制剂，可抑制 DDX3 的活性。

体外：RK-33 shows inhibition of many kinds of cancer cells with IC50 of 3-6 µM, while PC3 is much less sensitive to RK-33 (IC50 >12 µM). RK-33 treatment causes a significant accumulation in the G1 phase for DU145 and LNCaP, although treatment with RK-33 causes only a moderate accumulation of the G1 phase for 22Rv1, and the treated cells have significantly reduced G2 phase. RK-33 treatment also causes 12 moderate G1 accumulation in 22Rv1[1]. RK-33-loaded NPs demonstrate cytotoxicity to MCF-7 cells in a dose-dependent manner, while equivalent doses of empty NPs have no killing effect. The IC50 value of 5% RK-33 loaded NPs is 49 μg/mL, and the IC50 value of 10% RK-33 loaded NPs is 25 μg/mL[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内：There is more cell death (pyknotic or condensed nuclei) admixed with fibrin and interstitial edema in the tumors from mice from the combination RK-33 and radiation group compared to the control or single treatment groups. The treatment combination of RK-33 and radiation has an advantage in reducing tumor proliferation[1]. In the mice treated with RK-33-PLGA, RK-33 can be detected in the plasma (34 μg/mL) and liver (28 μg/g), but not lungs[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

细胞试验：简而言之，将8×102 MCF-7细胞接种在96孔板中，并在第二天用不同浓度的RK-33负载纳米粒子和未负载纳米粒子处理。孵育72小时后，将MTS试剂加入细胞中，并与MTS试剂孵育2小时后在490nm处测量吸光度。该实验独立重复三次。

动物体内实验:根据肿瘤生长情况，小鼠被随机重新分配为四组，每组八只，这导致在放射和 RK-33 药物治疗开始时肿瘤大小分布大致相等。盲选四组小鼠进行四种不同的实验程序，包括对照（仅注射DMSO）、RK-33治疗（仅注射RK-33 50 mg/kg）、放射（一次性放射5 Gy） ，或放疗和 RK-33 治疗（5 Gy 放疗和 RK-33 注射的组合）。 RK-33 和 DMSO 腹膜内注射，每周三次，持续两周。在药物注射开始时，使用小动物放射研究平台 (SARRP) 使用直径 1 厘米的圆形光束进行放射，聚焦于肿瘤部位。放射后0小时和24小时对每组小鼠实施安乐死，并提取肿瘤进行γH2AX、裂解的Caspase 3和Ki67染色。每组的其余小鼠均使用 Xenogen IVIS Spectrum 进行成像，并在成像前 5 分钟注射 D-荧光素。六周成像后对小鼠实施安乐死，并提取肿瘤进行 H&E 染色、裂解的 Caspase 3 和 i67 染色。兽医病理学家在苏木精和伊红染色切片上评估 RK-33 和放射治疗后肿瘤的形态。

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研究领域：Others

作用靶点：Others

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参考文献：[1]. Xie M,et al. RK-33 radiosensitizes prostate cancer cells by blocking the RNA helicase DDX3. Cancer Res. 2016 Sep 12.[2]. Bol GM, e tal. PLGA nanoparticle formulation of RK-33: an RNA helicase inhibitor against DDX3. Cancer Chemother Pharmacol. 2015 Oct;76(4):821-7.