BI 2536
Cat. No.：YN270402
CAS No. ：755038-02-9
| 产品名称: | BI 2536 |
| CAS No.: | 755038-02-9 |
| Chemical Name: | 4-[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide |
| Synonyms: | 4-[[(7R)-8-环戊基-7-乙基-5,6,7,8-四氢-5-甲基-6-氧代-2-喋啶基]氨基]-3-甲氧基-N-(1-甲基-4-哌啶基)苯甲酰胺 |
| 分子量: | 521.65 |
| 分子式: | C₂₈H₃₉N₇O₃ |
| SMILES: | O=C1[C@H](N(C2=C(N1C)C=NC(NC3=CC=C(C(NC4CCN(C)CC4)=O)C=C3OC)=N2)C5CCCC5)CC |
| 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: | BI 2536 是PLK1和BRD4的双抑制剂，IC50分别为 0.83 和 25 nM。BI-2536 抑制 IFNB (IFN-β，干扰素 β) 基因转录。 |
| IC50和靶点: | [{name:"PLK1:0.83 nM (IC50)"},{name: "Plk2/Snk:3.5 nM (IC50)"},{name: "Plk3/Fnk:9 nM (IC50)"},{name: "BRD4:25 nM (IC50)"}] |
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Schöffski, P.Polo-like kinase (PLK) inhibitors in preclinical and early clinical development in oncologyOncologist14(6),559-570(2009)
Steegmaier, M., Hoffmann, M., Baum, A., et al.BI 2536, a potent and selective inhibitor of polo-like kinase 1, inhibits tumor growth in vivoCurr. Biol.17(4),316-322(2007)
Peifer, C., and Alessi, D.R.Small-molecule inhibitors of PDK1ChemMedChem3(12),1810-1838(2008)
Danovi, D., Folarin, A., Gogolok, S., et al.A high-content small molecule screen identifies sensitivity of glioblastoma stem cells to inhibition of polo-like kinase 1PLoS One8(10),1-13(2013)
Ciceri, P., Müller, S., O'Mahony, A., et al.Dual kinase-bromodomain inhibitors for rationally designed polypharmacologyNat. Chem. Biol.10(4),305-312(2014)
