Onvansertib (NMS-P937) - 10mM in DMSO, high purity , CAS No.1034616-18-6

Item Number

O420423

• Synonyms: Onvansertib | 1034616-18-6 | NMS-1286937 | NMS-P937 | Onvansertib free base | NMS-P937 (NMS1286937) | Onvansertib [USAN] | PCM-075 | 1-(2-Hydroxyethyl)-8-((5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl)amino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamid
• Specifications & Purity: Moligand™, 10mM in DMSO
• Biochemical and Physiological Mechanisms: Onvansertib (NMS-P937, PCM-075, NMS1286937) is an orally available, selective Polo-like Kinase 1 (PLK1) inhibitor with IC50 of 2 nM, 5000-fold selectivity over PLK2/PLK3. Onvansertib (NMS-P937) potently causes a mitotic cell-cycle arrest followed by apopt
• Storage Temp: Store at -80°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™

Product Description

Information

Onvansertib (NMS-P937, PCM-075, NMS1286937) is an orally available, selectivePolo-like Kinase 1 (PLK1)inhibitor withIC50of 2 nM, 5000-fold selectivity over PLK2/PLK3. Onvansertib (NMS-P937) potently causes a mitotic cell-cycle arrest followed byapoptosisin cancer cell lines and inhibits tumor growth. Phase 1.

Targets

PLK1 2 nM

In vitro

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.

In vivo

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. 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.

Cell Research(from reference)

Cell lines：137 solid tumor cell lines, and 43 cell lines derived from leukemias and lymphomas 

Concentrations：~10 μM 

Incubation Time：72 hours