RGB-286638 free base
Cat. No.:YN340176
产品名称: | RGB-286638 free base |
CAS No.: | 784210-88-4 |
Chemical Name: | N-[1,4-dihydro-3-[4-[[4-(2-methoxyethyl)-1-piperazinyl]methyl]phenyl]-4-oxoindeno[1,2-c]pyrazol-5-yl]-N′-4-morpholinyl-urea |
Synonyms: | RGB-286638,RGB 286638,RGB-286638 |
分子量: | 545.63 |
分子式: | C₂₉H₃₅N₇O₄ |
SMILES: | O=C(NN1CCOCC1)NC2=CC=CC(C3=C4C(C5=CC=C(CN6CCN(CCOC)CC6)C=C5)=NN3)=C2C4=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: | RGB-286638 是一种有效的CDK抑制剂,抑制cyclin T1-CDK9,cyclin B1-CDK1,cyclin E-CDK2,cyclin D1-CDK4,cyclin E-CDK3和p35-CDK5活性,IC50分别为 1,2,3,4,5 和 5 nM;同时可抑制 GSK-3β,TAK1,Jak2 和 MEK1,IC50值分别为 3,5,50,和 54 nM。 |
IC50和靶点: | [{name:"T1-CDK9:1 nM (IC50)"},{name: "cyclin B1-CDK1:2 nM (IC50)"},{name: "cyclin E-CDK2:3 nM (IC50)"},{name: "cyclin D1-CDK4:4 nM (IC50)"},{name: "cyclin E-CDK3:5 nM (IC50)"},{name: "p35-CDK5:5 nM (IC50)"},{name: "cyclin H-CDK7:44 nM (IC50)"},{name: "cyclin D3-CDK6:55 nM (IC50)"},{name: "GSK-3β:3 nM (IC50)"},{name: "JAK2:50 nM (IC50)"},{name: "MEK1:54 nM (IC50)"},{name: "Fms:1 nM (IC50)"},{name: "TAK1:5 nM (IC50)"},{name: "JNK1a1:17 nM (IC50)"},{name: "JNK1a2:40 nM (IC50)"},{name: "C-src:25 nM (IC50)"},{name: "AMPK:41 nM (IC50)"}] |
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Cirstea, D., Hideshima, T., Santo, L., et al.Small-molecule multi-targeted kinase inhibitor RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKsLeukemia27(12),2366-2375(2013)