Midostaurin
Cat. No.：YN310057
CAS No. ：120685-11-2
| 产品名称: | Midostaurin |
| CAS No.: | 120685-11-2 |
| Chemical Name: | N-[(9S,10R,11R,13R)-2,3,10,11,12,13-hexahydro-10-methoxy-9-methyl-1-oxo-9,13-epoxy-1H,9H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-11-yl]-N-methyl-benzamide |
| Synonyms: | 米哚妥林; PKC412; CGP 41251 |
| 分子量: | 570.64 |
| 分子式: | C₃₅H₃₀N₄O₄ |
| SMILES: | O=C(C1=CC=CC=C1)N(C)[C@H]2[C@@H](OC)[C@@]3(C)N(C4=C5C=CC=C4)C6=C5C7=C(C(NC7)=O)C8=C6N(C9=CC=CC=C98)[C@@](O3)([H])C2 |
| 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: | Midostaurin (PKC412; CGP 41251) 是一种多靶点蛋白激酶抑制剂，抑制PKCα/β/γ，Syk，Flk-1，Akt，PKA，c-Kit，c-Fgr，c-Src，FLT3，PDFRβ和VEGFR1/2的IC50值范围为 22-500 nM。 |
| IC50和靶点: | [{name:"cPKC-α:22 nM (IC50)'}, 'eNOS', {'cPKC-γ:24 nM (IC50)"},{name: "cPKC-β1:30 nM (IC50)"},{name: "cPKC-β2:31 nM (IC50)"},{name: "nPKC-δ:33 nM (IC50)"},{name: "nPKC-η:160 nM (IC50)"},{name: "nPKC-ε:1250 nM (IC50)"},{name: "aPKC-ζ:465000 nM (IC50)"},{name: "PPK:38 nM (IC50)"},{name: "KDR:86 nM (IC50)"},{name: "c-Syk:95 nM (IC50)"},{name: "cdk1/cycB:570 nM (IC50)"},{name: "Protein kinase A:570 nM (IC50)"},{name: "c-Fgr:790 nM (IC50)"},{name: "c-Src:800 nM (IC50)"},{name: "Flt-1:912 nM (IC50)"},{name: "EGF-R:1100 nM (IC50)"},{name: "Myosin-light chain kinase:1900 nM (IC50)"},{name: "Flk-1:3900 nM (IC50)"},{name: "c-Lyn:4300 nM (IC50)"},{name: "P70S6 kinase:5000 nM (IC50)"},{name: "CSK:8000 nM (IC50)"}] |
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Fabbro, D., Buchdunger, E., Wood, J., et al.Inhibitors of protein kinases: CGP 41251, a protein kinase inhibitor with potential as an anticancer agentPharmacol. Ther.82(2-3),293-301(1999)
Ozaki, H., Seo, M.S., Ozaki, K., et al.Blockade of vascular endothelial cell growth factor receptor signaling is sufficient to completely prevent retinal neovascularizationAm. J. Pathol.156(2),697-707(2000)
Tenzer, A., Zingg, D., Rocha, S., et al.The phosphatidylinositide 3'-kinase/Akt survival pathway is a target for the anticancer and radiosensitizing agent PKC412, an inhibitor of protein kinase CCancer Res.61(22),8203-8210(2001)
Andrejauskas-Buchdunger, E., and Regenass, U.Differential inhibition of the epidermal growth factor-, platelet-derived growth factor-, and protein kinase C-mediated signal transduction pathways by the staurosporine derivative CGP 41251Cancer Res.52(19),5353-5358(1992)
Li, H., Hergert, S.M., Schäfer, S.C., et al.Midostaurin upregulates eNOS gene expression and preserves eNOS function in the microcirculation of the mouseNitric Oxide12(4),231-236(2005)
Marmy-Conus, N., Hannan, K.M., and Pearson, R.B.Ro 31-6045, the inactive analogue of the protein kinase C inhibitor Ro 31-8220, blocks in vivo activation of p70s6k/p85s6k: Implications for the analysis of S6K signallingFEBS Lett.519(1-3),135-140(2002)
El Fitori, J., Su, Y., Büchler, P., et al.PKC412 small-molecule tyrosine kinase inhibitor: Single-compound therapy for pancreatic cancerCancer110(7),1457-1468(2007)
