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NMS-P937(NMS1286937 Onvansertib)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
NMS-P937(NMS1286937 Onvansertib)图片
CAS NO:1034616-18-6
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)532.52
FormulaC24H27F3N8O3
CAS No.1034616-18-6
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 42 mg/mL (78.9 mM)
Water:<1 mg/mL
Ethanol: 10 mg/mL (18.8 mM)
SMILES O=C(C1=NN(CCO)C2=C1CCC3=CN=C(NC4=CC(N5CCN(C)CC5)=CC=C4OC(F)(F)F)N=C23)N
Synonyms NMS-P937; NMS1286937; NMS-P-937; NMS-P 937; NMS 1286937; NMS-1286937
实验参考方法
In Vitro

In vitro activity: NMS-P937 shows a broad-spectrum antiproliferative activity against different solid tumor, leukemias and lymphomas cell lines. NMS-P937 potently causes a mitotic cell-cycle arrest followed by apoptosis in A2780 cells.


Kinase Assay: 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 Supernatant, containing the phosphorylated substrate, is subsequently withdrawn and transferred into a counting plate, followed by evaluation by b-counting.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.


Cell Assay: Cells (137 solid tumor cell lines, and 43 cell lines derived from leukemias and lymphomas) 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.

In VivoIn 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. 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.
Animal model Mice xenografted with human HCT116 colon adenocarcinoma cells
Formulation & Dosage 90 mg/kg/d i.v. or p.o.
ReferencesBioorg Med Chem Lett. 2011 May 15;21(10):2969-74; Mol Cancer Ther. 2012 Apr;11(4):1006-16.