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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。
标签:NMS-1286937
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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.
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更新时间:2024/1/2 10:20:04
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