AZD2858
Cat. No.：YN420224
CAS No. ：486424-20-8
规格
价格(RMB)
库存
| 产品名称: | AZD2858 |
| CAS No.: | 486424-20-8 |
| Chemical Name: | 3-amino-6-[4-[(4-methyl-1-piperazinyl)sulfonyl]phenyl]-N-3-pyridinyl-2-pyrazinecarboxamide |
| Synonyms: | AZD2858;3-amino-6-[4-(4-methylpiperazin-1-yl)sulfonylphenyl]-N-pyridin-3-ylpyrazine-2-carboxamide;3-Amino-6-{4-[(4-methyl-1-piperazinyl)sulfonyl]phenyl}-N-(3-pyrid inyl)-2-pyrazinecarboxamide;AZD 2858;AZD-2858;AZD 2858;3-amino-6-(4-((4-methylpiperazin-1- |
| 分子量: | 453.52 |
| 分子式: | C₂₁H₂₃N₇O₃S |
| SMILES: | O=C(C1=NC(C2=CC=C(S(=O)(N3CCN(C)CC3)=O)C=C2)=CN=C1N)NC4=CC=CN=C4 |
| 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: | AZD2858 是一种有效的，可口服的GSK-3抑制剂，可以抑制GSK-3α和GSK-3β的活性，IC50值分别为 0.9 和 5 nM，可用于骨折愈合的研究。 |
| IC50和靶点: | [{name:"GSK-3α:0.9 nM (IC50)"},{name: "GSK-3β:5 nM (IC50)"},{name: "CDK5/p25:356 nM (IC50)"},{name: "Haspin:366 nM (IC50)"},{name: "CDK5/p35:387 nM (IC50)"},{name: "DYRK2:491 nM (IC50)"},{name: "CDK2/cyclin A:810 nM (IC50)"},{name: "CDK1/cyclin B:1246 nM (IC50)"},{name: "PIM3:1269 nM (IC50)"},{name: "TLK2:1381 nM (IC50)"},{name: "PKD2:2462 nM (IC50)"},{name: "CDK2/cyclin E:3310 nM (IC50)"},{name: "Aurora-A:4966 nM (IC50)"}] |
| In Vitro: | |
| In Vivo: | |
| Clinical Trial: | |
| Solvent & Solubility: |
Ring, D.B., Johnson, K.W., Henriksen, E.J., et al.Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivoDiabetes52(3),588-595(2003)
Asuni, A.A., Hooper, C., Reynolds, C.H., et al.GSK3α exhibits β-catenin and tau directed kinase activities that are modulated by WntEur. J. Neurosci.24(12),3387-3392(2006)
Phiel, C.J., Wilson, C.A., Lee, V.M., et al.GSK-3α regulates production of Alzheimer's disease amyloid-β peptidesNature423(6938),435-439(2003)
Guerrero, F., Herencia, C., Almadén, Y., et al.TGF-β prevents phosphate-induced osteogenesis through inhibition of BMP and Wnt/β-catenin pathwaysPLoS One9(2),e89179(2014)
Berg, S., Bergh, M., Hellberg, S., et al.Discovery of novel potent and highly selective glycogen synthase kinase-3ß (GSK3ß) inhibitors for Alzheimer's disease: Design, synthesis, and characterization of pyrazinesJ. Med. Chem.55(21),9107-9119(2012)
Marsell, R., Sisask, G., Nilsson, Y., et al.GSK-3 inhibition by an orally active small molecule increases bone mass in ratsBone50(3),619-627(2012)
Gilmour, P.S., O'Shea, P.J., Fagura, M., et al.Human stem cell osteoblastogenesis mediated by novel glycogen synthase kinase 3 inhibitors induces bone formation and a unique bone turnover biomarker profile in ratsToxicol. Appl. Pharmacol.272(2),399-407(2013)
