NMS-1286937 - CAS 1034616-18-6
Catalog number: 1034616-18-6
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C24H27F3N8O3
Molecular Weight:
532.528
COA:
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Targets:
Polo-like Kinase (PLK)
Description:
NMS1286937, also know as NMS-P937, is an 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.
Purity:
>98%
Appearance:
Solid powder
Synonyms:
PCM-075; PCM 075; PCM075; NMS1286937; NMS 1286937; NMS-1286937; NMS-P937; NMS-P-937; NMS-P 937; Onvansertib
MSDS:
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InChIKey:
QHLVBNKYJGBCQJ-UHFFFAOYSA-N
InChI:
InChI=1S/C24H27F3N8O3/c1-33-6-8-34(9-7-33)15-3-5-18(38-24(25,26)27)17(12-15)30-23-29-13-14-2-4-16-20(22(28)37)32-35(10-11-36)21(16)19(14)31-23/h3,5,12-13,36H,2,4,6-11H2,1H3,(H2,28,37)(H,29,30,31)
Canonical SMILES:
CN1CCN(CC1)C2=CC(=C(C=C2)OC(F)(F)F)NC3=NC=C4CCC5=C(C4=N3)N(N=C5C(=O)N)CCO
Current Developer:
Nerviano Medical Sciences.
1.Targeting polo-like kinase 1 by NMS-P937 in osteosarcoma cell lines inhibits tumor cell growth and partially overcomes drug resistance.
Sero V;Tavanti E;Vella S;Hattinger CM;Fanelli M;Michelacci F;Versteeg R;Valsasina B;Gudeman B;Picci P;Serra M Invest New Drugs. 2014 Dec;32(6):1167-80. doi: 10.1007/s10637-014-0158-6. Epub 2014 Sep 7.
BACKGROUND: ;Polo-like kinase 1 (PLK1) has emerged as a prognostic factor in various neoplasms, but only scarce data have been reported for high-grade osteosarcoma (OS). In this study, we assessed PLK1 expression and the efficacy of PLK1 inhibitor NMS-P937 in OS.;METHODS: ;PLK1 expression was assessed on 21 OS clinical samples and on a panel of human OS cell lines. In vitro efficacy of NMS-P937 was evaluated on nine drug-sensitive and six drug-resistant human OS cell lines, either as single agent or in combination with the drugs used in chemotherapy for OS.;RESULTS: ;PLK1 expression was higher in OS clinical samples and cell lines compared to normal human tissue. A higher PLK1 expression at diagnosis appeared to be associated with an unfavourable clinical outcome. PLK1 silencing produced growth inhibition, cell cycle retardation and apoptosis induction in human OS cell lines. NMS-P937 proved to be highly active in both drug-sensitive and drug-resistant cell lines, with the only exception of ABCB1-overexpressing, Doxorubicin (DX)-resistant variants. However, in these cells, the association of NMS-P937 with DX was able to revert DX-resistance by negatively interfering with ABCB1 transport activity.
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CAS 1034616-18-6 NMS-1286937

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