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抑制剂/激活剂

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凋亡与自噬

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Onvansertib NMS-1286937; NMS-P937

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

货号：
TK0259
规格：

1mg

2mg

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	1034616-18-6
生物活性	NMS-1286937 is a potent, selective and orally available PLK1 inhibitor, with an IC50 of 2 nM.
分子式	C24H27F3N8O3
分子量	532.52
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : 21 mg/mL (39.44 mM; Need ultrasonic and warming)
体内研究	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.
体外研究	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.
文献	•Science. 2017 Dec 1;358(6367):eaan4368. •Comput Struct Biotechnol J. 2019 Feb 8;17:352-361. •Sci Rep. 2017 Aug 17;7(1):8629. •Harvard Medical School LINCS LIBRARY
纯度及产品资料	98%

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