搜索

159-2642-3062

服务热线(工作日:9:00-17:30)

武汉科斯坦生物科技有限公司

热搜词:燕窝酸,不饱和脂肪酸,神经酰胺,花青素,黄酮,皂苷

Wuhan Chemstan Biotechnology Co., Ltd.

武汉科斯坦生物科技有限公司

代谢组学

科研服务

抗体/蛋白

地       址:武汉市东湖新技术开发区高新大道666号,武汉

                 国家生物产业基地B、C、D区研发楼C1栋
产品销售:15926423062
技术服务:18971263062                                             
E - mail :
info@chemstan.com       
邮       编:430075

化合物单体

科斯坦生物(Chemstan)所有产品和服务仅用于科学研究,不为任何个人或者非科研性质的用途提供产品和服务。

Copyright @ 武汉科斯坦生物科技有限公司.All rights reserved

网站建设:中企动力武汉鄂ICP备19006850号-1

浏览量:
产品名称:

NMS-P937

NO.
8
货号
CS6247
中文名称
NMS-P937
英文名称
NMS-P937
CAS号
1034616-18-6
产品货号:
CS6247
货期:
现货
价格与订购:
150.00
数量
-
+
库存
300
没有此类产品
产品信息
如何订购
产品描述icon
NMS-P937 (NMS1286937), an oral, specific Polo-like Kinase 1 (PLK1) inhibitor, is with IC50 of 2 nM. The specificity of NMS-P937 forPLK1 is 5000-fold higher over PLK2/PLK3.
靶点活性icon
PLK1    PLK2    PLK3
体外活性icon
In M-NFS-60, Bac1.2F5 and M-07e cells, Pexidartinib inhibits the CSF1-dependent proliferation with IC50 of 0.44 μM, 0.22 μMand 0.1 μM, respectively. [1]
体内活性icon
In mice xenografted with human HCT116 colon adenocarcinoma cells, NMS-P937 (90 mg/kg/d i.v. or p.o.) shows a significant tumor growth inhibition. [1] In mice bearing HT29, Colo205 colorectal, or A2780 ovarian xenograft tumors, NMS-P937 inhibits xenograft tumor growth. In addition, NMS-P937, in combination with approved cytotoxic drugs, causes enhanced tumor regression, and prolongs survival of animals. [2]
激酶实验icon
Kinase profile: The inhibitory activity of putative kinase inhibitors and the potency of selected compounds are determined using a trans-phosphorylation assay. Specific peptide or protein substrates are trans-phosphorylated by their specific serine-threonine or tyrosine kinase, in the presence of ATP traced with 33P-γ-ATP, at optimized buffer and cofactors conditions. At the end of the phosphorylation reaction, more than 98% unlabeled ATP and radioactive ATP is captured by adding an excess of the ion exchange dowex resin; the resin then settles down to the bottom of the reaction plate by gravity. Supernatant, containing the phosphorylated substrate, is subsequently withdrawn and transferred into a counting plate, followed by evaluation by b-counting. Inhibitory potency evaluation for all the tested kinases was performed at 25 °C using a 60 min end-point assay where the concentrations of ATP and substrates are kept equal to 2 x αKm and saturated (>5 x αKm), respectively.
细胞实验icon
Cells are seeded into 96- or 384-well plates at densities ranging from 10,000 to 30,000/cm2 for adherent and 100,000/mL for nonadherent cells in appropriate medium supplemented with 10% fetal calf serum. After 24 hours, cells were treated in duplicate with serial dilutions of NMS-P937, and 72 hours later, the viable cell number was assessed by the CellTiter-Glo Assay (Promega). IC50 values were calculated with a sigmoidal fitting algorithm (Assay Explorer MDL). Experiments were carried out independently at least twice.(Only for Reference) Cell lines: 137 solid tumor cell lines, and 43 cell lines derived from leukemias and lymphomasicon
参考文献icon
1. Beria I, et al. Bioorg Med Chem Lett. 2011, 21(10), 2969-2974.2. Valsasina B, et al. Mol Cancer Ther. 2012, 11(4), 12006-12016.
别名icon
NMS-1286937 , NMS-1286937
纯度icon
99.88%
分子量icon
532.52
分子式icon
C24H27F3N8O3
CAS Noicon
1034616-18-6
存储icon
0-4℃ for short term (days to weeks), or -20℃ for long term (months).
溶解度
icon
DMSO: 39 mg/mL (73.2 mM)
Ethanol: 10 mg/mL (18.77 mM), warmed
Water: <1 mg/mL
( < 1 mg/ml refers to the product slightly soluble or insoluble )
icon
Note
icon
For research use only .
未找到相应参数组,请于后台属性模板中添加
暂未实现,敬请期待
暂未实现,敬请期待
上一篇
下一篇