S81196
- 公司名稱 上海源葉生物科技有限公司
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- 廠商性質(zhì) 生產(chǎn)廠家
- 更新時(shí)間 2025/5/15 20:10:44
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- 產(chǎn)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.
- 靶點(diǎn)： PLK1
- 體外研究： 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.
- 體內(nèi)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.
- 參考文獻(xiàn)：
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 超聲可增加溶解度
母液保存：分裝凍存，避免反復(fù)凍融；-20℃，1個(gè)月；-80℃，6個(gè)月（稀釋后溶液溫度低保存可能會(huì)析出，盡量現(xiàn)用現(xiàn)配）
細(xì)胞實(shí)驗(yàn):先用DMSO溶解：再用培養(yǎng)基進(jìn)行稀釋，稀釋過(guò)程建議分段進(jìn)行，避免濃度變化過(guò)快導(dǎo)致化合物析出。若稀釋過(guò)程中出現(xiàn)化合物析出的情況， 可采用超聲的方法使其復(fù)溶。在稀釋時(shí)要確保工作液中 DMSO 的終濃度盡量在0.1%以下，不要超過(guò)0.5%，并設(shè)置相應(yīng)濃度的DMSO對(duì)照組。
動(dòng)物實(shí)驗(yàn)：先用DMSO溶解：再用水或者生理鹽水等去稀釋，稀釋過(guò)程建議分段進(jìn)行，避免濃度變化過(guò)快導(dǎo)致化合物析出。若稀釋過(guò)程中出現(xiàn)化合物析出的情況， 可采用超聲的方法使其復(fù)溶?？梢酝ㄟ^(guò)添加助溶劑來(lái)幫助溶解，比如植物油、Tween80、甘油、羧甲基纖維素鈉和PEG400等。具體方式請(qǐng)參考文獻(xiàn)。懸濁液可用于口服和腹腔注射，不會(huì)影響產(chǎn)品活性。
- 保存條件： -20℃
- 配置溶液濃度參考：
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：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的性，僅供客戶參考交流研究之用。
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