Niraparib tosylate
Cat. No.：YN270068
CAS No. ：1038915-73-9
| 产品名称: | Niraparib tosylate |
| CAS No.: | 1038915-73-9 |
| Chemical Name: | 2-[4-(3S)-3-piperidinylphenyl]-2H-indazole-7-carboxamide, 4-methylbenzenesulfonate |
| Synonyms: | 尼拉帕尼对苯甲磺酸盐; MK-4827 tosylate |
| 分子量: | 492.59 |
| 分子式: | C₂₆H₂₈N₄O₄S |
| SMILES: | NC(C1=CC=CC2=CN(C3=CC=C([C@H]4CNCCC4)C=C3)N=C21)=O.O=S(C5=CC=C(C)C=C5)(O)=O |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | Niraparib tosylate (MK-4827 tosylate) 是一种高效的，具有生物口服利用度的PARP1和PARP2抑制剂，IC50分别为 3.8 和 2.1 nM。Niraparib tosylate 抑制 DNA 损伤修复，诱导凋亡 (apoptosis) 并具有抗肿瘤活性。 |
| IC50和靶点: | [{name:"PARP-2:2.1 nM (IC50)"},{name: "PARP-1:3.8 nM (IC50)"},{name: "V-PARP:330 nM (IC50)"},{name: "TANK-1:570 nM (IC50)"},{name: "PARP-3:1300 nM (IC50)"}] |
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Jones, P., Altmura, S., Boueres, J., et al.Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): A novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumorsJ. Med. Chem.52(22),7170-7185(2009)
Yuan, Y., Liao, Y.M., Hsueh, C.T., et al.Novel targeted therapeutics: Inhibitors of MDM2, ALK and PARPJ. Hematol. Oncol.4(16),1-14(2011)
Wang, L., Mason, K.A., Ang, K.K., et al.MK-4827, a PARP-1/-2 inhibitor, strongly enhances response of human lung and breast cancer xenografts to radiationInvest New Drugs30(6),2113-2120(2012)
Mirza, M.R., Monk, B.J., Herrstedt, J., et al.Niraparib maintenance therapy in platinum-sensitive, recurrent ovarian cancerN. Engl. J. Med.375(22),2154-2164(2016)
