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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.
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