 |
上海源叶生物科技有限公司
主营产品： S30260异硫氰酸胍,30259盐酸胍,嗜热菌蛋白酶 |
联系电话
15921386130
公司信息
- 联系人：
- 何小姐
- 电话：
- 86-021-61559134
- 手机：
- 15921386130
- 传真：
- 86-021-55068248
- 地址：
- 上海市松江区长塔路465号6幢
- 邮编：
- 200433
- 网址：
- www.shyuanye.com
| 参考价 | 面议 |
- 型号
- 品牌
- 厂商性质 生产商
- 所在地
更新时间：2025-05-15 20:10:44浏览次数：132
联系我们时请说明是化工仪器网上看到的信息，谢谢!
- 提示：详情请下载说明书。
- 产品描述：
RO3280, also known as Ro5203280, is a potent and selective PLK 1 inhibitor with excellent in vitro cellular potency. RO3280 showed strong antitumor activity in xenograft mouse models. he 50% inhibitory concentration (IC50) of RO3280 for acute leukemia cells was between 74 and 797 nM. The IC50 of RO3280 in primary acute lymphocytic leukemia (ALL) and AML cells was between 35.49 and 110.76 nM and 52.80 and 147.50 nM, respectively. RO3280 induced apoptosis and cell cycle disorder in leukemia cells. RO3280 treatment regulated several apoptosis-associated genes. Polo-like kinase 1 (PLK1) is highly expressed in many cancers and therefore a biomarker of transformation and potential target for the development of cancer-specific small molecule drugs.
- 靶点： PLK1
- 体外研究： Ro3280 (RO3280) inhibits PLK1 activity in NB4 and K562 cells, with an IC50s of 13.45 nM and 301 nM, respectively. RO3280 shows inhibitory activities against the growth of six leukemia cells, with IC50s of 186 nM, 175 nM, 74 nM, 797 nM, 120 nM and 162 nM for U937, HL60, NB4, K562, MV4-11 and CCRF cell lines, respectively. RO3280 also suppresses the growth of primary ALL and AML cells, with IC50s of 35.49-110.76 nM, and 52.80-147.50 nM, respectively. RO3280 (50 or 100 nM) induces apoptosis and cell cycle disorder in acute leukemia cells. Ro3280 shows potent activity in H82, H69, A549 lung cancer cell lines with EC50s of 6 nM, 7 nM and 82 nM. Ro3280 also inhibits several other cancer cell lines, with low concentration. RO3280 is cytotoxic to 5637 and T24 human bladder cancer cells, with IC50s of appr 100 nM.
- 体内研究： Ro3280 (RO3280, 40 mg/kg, i.v.) inhibits 72% tumor growth in a mouse xenograft model implanted with HT-29 colorectal cancer cells, and when dosed more frequently, RO3280 completely suppresses the tumor growth. RO3280 (30 mg/kg, once every 5 days, i.p.) shows significant anti-bladder cancer activities in a nude mouse model.
- 参考文献：
1. Wang NN, et al. Molecular targeting of the oncoprotein PLK1 in pediatric acute myeloid leukemia: RO3280, a novel PLK1 inhibitor, induces apoptosis in leukemia cells. Int J Mol Sci. 2015 Jan 7;16(1):1266-92.
2. Chen S, et al. Identification of novel, potent and selective inhibitors of Polo-like kinase 1. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1247-50.
3. Zhang Z, et al. Targeted inhibition of Polo-like kinase 1 by a novel small-molecule inhibitor induces mitotic catastrophe and apoptosis in human bladder cancer cells. J Cell Mol Med. 2017 Apr;21(4):758-767.
- 溶解度： DMSO : 80 mg/mL 超声可增加溶解度
母液保存：分装冻存，避免反复冻融；-20℃，1个月；-80℃，6个月（稀释后溶液温度低保存可能会析出，尽量现用现配）
细胞实验:先用DMSO溶解：再用培养基进行稀释，稀释过程建议分段进行，避免浓度变化过快导致化合物析出。若稀释过程中出现化合物析出的情况， 可采用超声的方法使其复溶。在稀释时要确保工作液中 DMSO 的终浓度尽量在0.1%以下，不要超过0.5%，并设置相应浓度的DMSO对照组。
动物实验：先用DMSO溶解：再用水或者生理盐水等去稀释，稀释过程建议分段进行，避免浓度变化过快导致化合物析出。若稀释过程中出现化合物析出的情况， 可采用超声的方法使其复溶?？梢酝ü砑又芗晾窗镏芙猓热缰参镉?、Tween80、甘油、羧甲基纤维素钠和PEG400等。具体方式请参考文献。悬浊液可用于口服和腹腔注射，不会影响产品活性。
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 1.84 ml 9.198 ml 18.396 ml 5 mM 0.368 ml 1.84 ml 3.679 ml 10 mM 0.184 ml 0.92 ml 1.84 ml 50 mM 0.037 ml 0.184 ml 0.368 ml
- 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的性，仅供客户参考交流研究之用。
