Onvansertib (NMS-P937, PCM-075, NMS1286937)是一种口服有效的，选择性的 Polo-like Kinase 1 (PLK1) 抑制剂,其IC50值为2 nM，比PLK2/PLK3高出5000倍的选择性。Onvansertib (NMS-P937) 可在肿瘤细胞系中造成有丝分裂周期阻滞及凋亡并抑制肿瘤生长。 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
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Onvansertib (NMS-P937)
Dangerous GoodsCAS number：1034616-18-6 molecular formula：C24H27F3N8O3
overview
compound introduction
Specs
| Chinese alias | 4,5-二氢-1-(2-羟基乙基)-8-[[5-(4-甲基-1-哌嗪基)-2-(三氟甲氧基)苯基]氨基]-1H-吡唑并[4,3-h]喹唑啉-3-甲酰胺 | 昂凡塞替尼 (NMS-P937) | ||
| English alias | 1-(2-Hydroxyethyl)-8-((5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl)amino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | BCP28066 | NMS-P937 | SB16941 | 1-(2-hydroxyethyl)-8-(5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)anilino)-4,5 | ||
| CAS number | 1034616-18-6 | molecular formula | C24H27F3N8O3 |
| molecular weight | 532.52 g/mol | Exact mass | - |
| PSA | 135.000 Ų | logp | 2 |
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physicochemical properties
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Safety information
pictogram：
GHS07
Signal word：
Warning
Hazard Statement：
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激 H302: 吞食有害
Statement of Preventive Measures：
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。
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