| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| O420423-1ml |
1ml |
现货  |
|
| 别名 | 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) |
|---|---|
| 英文别名 | 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 |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Onvansertib (NMS-P937) |
| 生化机理 | Onvansertib（NMS-P937，PCM-075，NMS1286937）是一种口服选择性Polo-like Kinase 1（PLK1）抑制剂，IC50为2 nM，比PLK2/PLK3的选择性高5000倍。Onvansertib（NMS-P937）能有效导致癌细胞系的有丝分裂细胞周期停滞，随后细胞凋亡，并抑制肿瘤生长。第一阶段 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 丝氨酸/苏氨酸蛋白激酶 PLK1 抑制剂 |
| 产品介绍 |
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 |
| ALogP | 2 |
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| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
| 分子类型 | 小分子 |
|---|---|
| IUPAC Name | 1-(2-hydroxyethyl)-8-[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)anilino]-4,5-dihydropyrazolo[4,3-h]quinazoline-3-carboxamide |
| 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) |
| InChi Key | QHLVBNKYJGBCQJ-UHFFFAOYSA-N |
| 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 |
| Isomeric SMILES | CN1CCN(CC1)C2=CC(=C(C=C2)OC(F)(F)F)NC3=NC=C4CCC5=C(C4=N3)N(N=C5C(=O)N)CCO |
| 分子量 | 532.52 |
| Reaxy-Rn | 18395773 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=18395773&ln= |
| 分子量 | 532.500 g/mol |
|---|---|
| XLogP3 | 2.000 |
| 氢键供体数Hydrogen Bond Donor Count | 3 |
| 氢键受体数Hydrogen Bond Acceptor Count | 12 |
| 可旋转键计数Rotatable Bond Count | 7 |
| 精确质量Exact Mass | 532.216 Da |
| 单同位素质量Monoisotopic Mass | 532.216 Da |
| 拓扑极表面积Topological Polar Surface Area | 135.000 Ų |
| 重原子数Heavy Atom Count | 38 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 817.000 |
| 同位素原子数Isotope Atom Count | 0 |
| 定义的原子立体中心计数Defined Atom Stereocenter Count | 0 |
| 未定义的原子立体中心计数Undefined Atom Stereocenter Count | 0 |
| 定义的键立体中心计数Defined Bond Stereocenter Count | 0 |
| 未定义的键立体中心计数Undefined Bond Stereocenter Count | 0 |
| 所有立体化学键的总数The total count of all stereochemical bonds | 0 |
| 共价键合单元计数Covalently-Bonded Unit Count | 1 |
| 象形图 | GHS07 |
|---|---|
| 信号词 | Warning |
| 危险声明 |
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 |
| 预防措施声明 |
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。 |
| Reaxy-Rn | 18395773 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=18395773&ln= |
| Concentration(Compounding value) | 9.0-11.0(mmol/L) |
|---|---|
| Appearance(Yellow-green Liquid) | Pass |
| Record the entire process by video | Conform |
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