NMS-P937( PCM-075 | PCM 075 | NMS1286937 )

Catalog No. M17767 CAS No. 1034616-18-6

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

NMS-P937
Note

Research use only, not for human use.
Brief Description

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.
Description

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.
In Vitro

——
In Vivo

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Synonyms

PCM-075 | PCM 075 | NMS1286937
Pathway

Others
Target

Other Targets
Recptor

PLK1| PLK2| PLK3
Research Area

Cancer
Indication

——

CAS Number

1034616-18-6
Formula Weight

532.52
Molecular Formula

C24H27F3N8O3
Purity

>98% (HPLC)
Solubility

DMSO : 21 mg/mL. 39.44 mM;
SMILES

CN1CCN(CC1)c1cc(c(cc1)OC(F)(F)F)Nc1ncc2CCc3c(c2n1)n(nc3C(=O)N)CCO
Chemical 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

1. Beria I, et al. Bioorg Med Chem Lett. 2011, 21(10), 2969-2974.

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