Ro3280
Cat. No.：YN290333
CAS No. ：1062243-51-9
| 产品名称: | Ro3280 |
| CAS No.: | 1062243-51-9 |
| Chemical Name: | 4-[(9-cyclopentyl-7,7-difluoro-6,7,8,9-tetrahydro-5-methyl-6-oxo-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide |
| Synonyms: | Ro5203280 |
| 分子量: | 543.61 |
| 分子式: | C₂₇H₃₅F₂N₇O₃ |
| SMILES: | COC1=C(NC2=NC(N(C3CCCC3)CC(F)(F)C(N4C)=O)=C4C=N2)C=CC(C(NC5CCN(C)CC5)=O)=C1 |
| 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: | Ro3280 是一种有效的，高度选择性的PLK1抑制剂，IC50和Kd值分别为 3 nM 和 0.09 nM，对 PLK2 和 PLK3 几乎没作用。 |
| IC50和靶点: | [{name:"PLK1:0.09 nM (Kd)"},{name: "ALK:230 nM (Kd)"},{name: "CAMKK1:1100 nM (Kd)"},{name: "CAMKK2:87 nM (Kd)"},{name: "DAPK1:100 nM (Kd)"},{name: "DAPK3:70 nM (Kd)"},{name: "FER:53 nM (Kd)"},{name: "GAK:87 nM (Kd)"},{name: "MYLK:170 nM (Kd)"},{name: "PTK2:84 nM (Kd)"},{name: "PTK2B:130 nM (Kd)"},{name: "RPS6KA6 (KinDom.2):560 nM (Kd)"},{name: "TTK:51 nM (Kd)"}] |
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Chen, S., Bartkovitz, D., Cai, J., et al.Identification of novel, potent and selective inhibitors of Polo-like kinase 1Bioorg. Med. Chem. Lett.22(2),1247-1250(2012)
Tao, Y.-F., Li, Z.-H., Du, W.-W., et al.Inhibiting PLK1 induces autophagy of acute myeloid leukemia cells via mammalian target of rapamycin pathway dephosphorylationOncol. Rep.37(3),1419-1429(2017)
Zhang, Z., Zhang, G., and Kong, C.Targeted inhibition of Polo-like kinase 1 by a novel small-molecule inhibitor induces mitotic catastrophe and apoptosis in human bladder cancer cellsJ. Cell. Mol. Med.21(4),758-767(2017)
Wang, N.-N., Li, Z.-H., Zhao, H., et al.Molecular targeting of the oncoprotein PLK1 in pediatric acute myeloid leukemia: RO3280, a novel PLK1 inhibitor, induces apoptosis in leukemia cellsInt. J. Mol. Sci.16(1),1266-1292(2015)
