产品中心

Onvansertib

型号:

产品价格:电议      采购度:1309      原产地:美洲

发布时间:2022/1/22 1:25:43      所属地区:国外 国外

简要描述:

nMS-1286937 是一种有效、高选择性、可口服的 PLK1 抑制剂,IC50 值为 2 nM。

产品咨询 服务电话:
021-58955995
分享到:

标签:NMS-1286937   

产品详情

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务。

Onvansertib

CAS No. : 1034616-18-6

MCE 站:Onvansertib

产品活性:nMS-1286937 是一种有效、高选择性、可口服的 PLK1 抑制剂,IC50 值为 2 nM。

研究领域:Cell Cycle/DNA Damage  |  Apoptosis

作用靶点:Polo-like Kinase (PLK)  |  Apoptosis

In Vitro: NMS-1286937 is a potent, selective and orally available PLK1 inhibitor, with IC50 of 2 nM. NMS-1286937 also shows inhibitory activities against FLT3, MELK, and CK2, with IC50s of 510, 744, and 826 nM, respectively. NMS-P937 possesses a pure ATP competitive mechanism with a reversible dissociation and no time dependency. NMS-P937 (10 μM) is selective with a marginal activity of 48% and 40% inhibition on PLK2 and PLK3, respectively. NMS-P937 shows antiproliferative activity against a panel of 137 cell lines, with IC50 values of below 100 nM for 60 of 137 cell lines and higher than 1 μM for only 9 of 137 cell lines. NMS-P937 shows cytotoxic activity against AmL-NS8 cells with IC50 of 36 nM.

In Vivo: NMS-1286937 (45 mg/kg, i.v.) shows a good tumor growth inhibition with acceptable and reversible body weight loss in CD1 nu/nu mice xenografted with human HCT116 colon adenocarcinoma cells. NMS-1286937 (60 mg/kg, p.o.) also inhibits the growth of tumor on HCT116 xenograft model. NMS-P937 (45 mg/kg, i.v.or 60 mg/kg, p.o) inhibits tumor growth to a comparable degree (TGI, 83% and 79% intravenously and orally, respectively) in HCT116-bearing mice. The combination of NMS-P937 (120 mg/kg given for 4 cycles of 2 consecutive days with 10-day rest) and cytarabine (75 mg/kg for 4 cycles of 5 consecutive days with 7-day rest) in the disseminated leukemia model AmL-PS is well tolerated and clearly showed increased mice survival. NMS-P937 (60 mg/kg bid os per day over 2 days with a 5 day rest) shows good efficacy compared to standard therapies, with a significant increase in median survival time (MST) in the established disease setting.

相关产品:Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Apoptosis Compound Library  |  Cell Cycle/DNA Damage Compound Library  |  Kinase Inhibitor Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Orally Active Compound Library  |  Anti-Blood Cancer Compound Library  |  Targeted Diversity Library  |  MG-132  |  LY294002  |  Doxorubicin hydrochloride  |  Bafilomycin A1  |  Y-27632 dihydrochloride  |  Paclitaxel  |  Angiotensin II human  |  Acetylcysteine  |  Staurosporine  |  Tamoxifen  |  5-Fluorouracil  |  Bortezomib  |  Sorafenib  |  2-Deoxy-D-glucose  |  Trametinib  |  SP600125  |  Gemcitabine  |  Temozolomide  |  MK-2206 dihydrochloride  |  Verteporfin  |  Decitabine  |  Etoposide  |  CCCP  |  Actinomycin D  |  DAPT  |  Pexidartinib  |  BAY 11-7082  |  Rotenone  |  Ruxolitinib

热门产品线:重组蛋白  |  化合物库  |  天然产物  |  染料试剂  |  PROTAC  |  同位素标记物

Trending products:Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物,我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物;
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域;
•   设有专业的实验中心和严格的质控、验证体系;
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告,确保产品的高纯度、高品质;
•   产品的生物活性多经各国客户实验验证;
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果;
•   专业团队跟踪*新的制药及生命科学研究进展,为您提供全球*新的活性化合物;
•   与世界各大制药公司及知名科研机构建立了长期的合作。

1000+ Inhibitors&Agonists 作用于20多条经典信号通路
30+ Screening Libraries 疾病机制研究的高效工具
CCK8 Kit | Cell Counting Kit-8
FDA-Approved 药物筛选库
Inhibitor Cocktails 蛋白酶, 磷酸酶 & 去乙酰化酶
Top Publications Citing Use of MCE
MCE Hotline: 4008203792 | 中国现货 - 全球文献引用 - 高纯度高品质 - 全方位技术支持

更新时间:2024/1/2 10:20:04

留言咨询

  •  
  •  
  •  
  •  
  •  
  •  
  •  
验证码: 点击切换验证码

温馨提示

1.遵守中华人民共和国有关法律、法规,尊重网上道德,承担一切因您的行为而直接或间接引起的法律责任。
2.请您真实的反映产品的情况,不要捏造、诬蔑、造谣。如对产品有任何疑问,也可以留言咨询。
3.未经本站同意,任何人不得利用本留言簿发布个人或团体的具有广告性质的信息或类似言论。

相关新闻

相关产品

联系我们

电话:021-58955995
传真:021-53700325
邮箱:sales@medchemexpress.cn
地址:上海上海

版权所有©MedChemExpress, All Right Reseverd ICP备案号: 总访问量:10864069 管理登录 阿仪网 设计制作,未经允许翻录必究

8

阿仪网推荐收藏该企业网站

联系方式

18019480960
18019480960

工作时间

(24小时)