Dacinostat
Cat. No.：YN280063
| 产品名称: | Dacinostat |
| CAS No.: | 404951-53-7 |
| Chemical Name: | (2E)-N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2-propenamide |
| Synonyms: | NVP-LAQ824; LAQ824 |
| 分子量: | 379.45 |
| 分子式: | C₂₂H₂₅N₃O₃ |
| SMILES: | O=C(NO)/C=C/C1=CC=C(CN(CCO)CCC2=CNC3=C2C=CC=C3)C=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: | Dacinostat 是一种有效的HDAC抑制剂，IC50值为 32 nM；Dacinostat 同时可抑制HDAC1的活性，IC50值为 9 nM，主要用于癌症研究。 |
| IC50和靶点: | [{name:"HDAC1:9 nM (IC50)"},{name: "HDAC:32 nM (IC50)"}] |
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Catley, L., Weisberg, E., Tai, Y.T., et al.NVP-LAQ824 is a potent novel histone deacetylase inhibitor with significant activity against multiple myelomaBlood102(7),2615-2622(2003)
Dokmanovic, M., Clarke, C., and Marks, P.A.Histone deacetylase inhibitors: Overview and perspectivesMol. Cancer Res.5(10),981-989(2007)
Zheng, Y.G., Wu, J., Chen, Z., et al.Chemical regulation of epigenetic modifications: Opportunities for new cancer therapyMed. Res. Rev.28(5),645-687(2008)
Rosato, R.R., Almenara, J.A., Maggio, S.C., et al.Role of histone deacetylase inhibitor-induced reactive oxygen species and DNA damage in LAQ-824/fludarabine antileukemic interactionsMol. Cancer Ther.7(10),3285-3297(2008)
Nimmanapalli, R., Fuino, L., Bali, P., et al.Histone deacetylase inhibitor LAQ824 both lowers expression and promotes proteasomal degradation of Bcr-Abl and induces apoptosis of imatinib mesylate-sensitive or -refractory chronic myelogenous leukemia-blast crisis cellsCancer Res.63(16),5126-5135(2003)
Fiskus, W., Ren, Y., Mohapatra, A., et al.Hydroxamic acid analogue histone deacetylase inhibitors attenuate estrogen receptor-α levels and transcriptional activity: A result of hyperacetylation and inhibition of chaperone function of heat shock protein 90Clin. Cancer Res.13(16),4882-4890(2007)
de Bono, J.S., Kristeleit, R., Tolcher, A., et al.Phase I pharmacokinetic and pharmacodynamic study of LAQ824, a hydroxamate histone deacetylase inhibitor with a heat shock protein-90 inhibitory profile, in patients with advanced solid tumorsClin. Cancer Res.14(20),6663-6673(2008)
