ONVANSERTIB

ONVANSERTIB - Names and Identifiers

Name	1-(2-hydroxyethyl)-8-((5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl)amino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
Synonyms	CS-1243 NMS-P937 NMS-1286937 ONVANSERTIB NMS-1286937,NMS-P937 NMS-P937 (NMS1286937) 1-(2-hydroxyethyl)-8-[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)anilino]-4,5-dihydropyrazolo[4,3-h]quinazoline-3-carboxamide 1-(2-hydroxyethyl)-8-((5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl)amino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide 4,5-Dihydro-1-(2-hydroxyethyl)-8-[[5-(4-methyl-1-piperazinyl)-2-(trifluoromethoxy)phenyl]amino]-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide 1H-Pyrazolo[4,3-h]quinazoline-3-carboxamide, 4,5-dihydro-1-(2-hydroxyethyl)-8-[[5-(4-methyl-1-piperazinyl)-2-(trifluoromethoxy)phenyl]amino]-
CAS	1034616-18-6

ONVANSERTIB - Physico-chemical Properties

Molecular Formula	C24H27F3N8O3
Molar Mass	532.52
Density	1.57±0.1 g/cm3(Predicted)
Boling Point	757.8±70.0 °C(Predicted)
Solubility	DMSO: 21 mg/mL
pKa	14.29±0.10(Predicted)
Storage Condition	-20℃
Use	Onvansertib, also know as NMS-P937, PCM-075 and NMS1286937, is a n orally bioavailable, small-molecule Polo-like kinase 1 (PLK1) inhibitor with potential antineoplastic activity. Polo-like kinase 1 inhibitor NMS-1286937 selectively inhibits PLK1, inducing selective G2/M cell-cycle arrest followed by apoptosis in a variety of tumor cells while causing reversible cell-cycle arrest at the G1 and G2 stages without apoptosis in normal cells. PLK1 inhibition may result in the inhibition of proliferation in PLK1-overexpressing tumor cells. PLK1 is a serine/threonine protein kinase crucial in the regulation of mitosis.
Target	PLK1；MELK；CK2；FLT3
In vitro study	NMS-P937 showed broad spectrum antiproliferative activity against different solid tumor, leukemia and lymphoma cell lines. NMS-P937 effectively causes mitotic cell cycle arrest in A2780 cells, leading to apoptosis.
In vivo study	In mice xenografted with human HCT116 colon cancer cells, nms-p937 (90 mg/kg/d I. v. Or p.o.) showed significant tumor growth inhibition. In mice bearing HT29,Colo205 colorectal cancer, or A2780 ovarian cancer xenografts, NMS-P937 inhibited the growth of the xenografts. In addition, NMS-P937, in combination with an approved cytotoxic drug, promotes tumor regression and prolongs the survival time of the animals.

ONVANSERTIB - Reference

Reference

1. Beria I, et al. NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor. Bioorg Med Chem Lett. 2011 May 15;21(10):2969-74.2. Valsasina B, et al. NMS-P937, an orally available, specific small-molecule polo-like kinase 1 inhibitor with antitumor activity in solid and hematologic malignancies. Mol Cancer Ther. 2012 Apr;11(4):1006-16.3. Casolaro A, et al. The Polo-Like Kinase 1 (PLK1) inhibitor NMS-P937 is effective in a new model of disseminated primary CD56+ acute monoblastic leukaemia. PLoS One. 2013;8(3):e58424.

ONVANSERTIB - Preparation solution concentration reference

	1mg	5mg	10mg
1 mM	1.878 ml	9.389 ml	18.779 ml
5 mM	0.376 ml	1.878 ml	3.756 ml
10 mM	0.188 ml	0.939 ml	1.878 ml
5 mM	0.038 ml	0.188 ml	0.376 ml

Last Update：2024-01-02 23:10:35

ONVANSERTIB - Reference Information

biological activity	NMS-P937(NMS1286937) is an orally active, selective Polo-like Kinase 1 (PLK1) the inhibitor has an IC50 of 2 nM, which is 5000 times more selective than PLK2/plk3. Stage 1. onvan sertib (NMS-P937, PCM-075, NMS1286937) is an orally potent, selective, Polo-like Kinase 1 (PLK1) inhibitor with an IC50 value of 2 nM, the selectivity was 5000 times higher than that of PLK2/plk3. Onvan sertib (NMS-P937) causes mitotic cycle arrest and apoptosis and inhibits tumor growth in tumor cell lines. Phase 1.
Target	Value
PLK1 ()	2 nM

Last Update：2024-04-09 21:04:16