Orantinib
Cat. No.:YN440102
产品名称: | Orantinib |
CAS No.: | 252916-29-3 |
Chemical Name: | 5-[(1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-propanoic acid |
Synonyms: | SU6668; TSU-68 |
分子量: | 310.35 |
分子式: | C₁₈H₁₈N₂O₃ |
SMILES: | CC1=C(/C=C2C3=CC=CC=C3NC/2=O)NC(C)=C1CCC(O)=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: | Orantinib (SU6668; TSU-68) 是多靶点的受体酪氨酸激酶抑制剂,对Flt-1,PDGFRβ和FGFR1的Ki值分别为 2.1 μM,8 nM 和 1.2 μM。 |
IC50和靶点: | [{name:"PDGFRβ:8 nM (Ki)"},{name: "FGFR1:1.2 μM (Ki)"},{name: "Flt-1:2.1 μM (Ki)"}] |
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Sun, L., Tran, N., Liang, C., et al.Design, synthesis, and evalutaions of substituted 3-[(3- or 4-carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as inhibitors of VEGF, FGF, and PDGF receptor tyrosine kinasesJ. Med. Chem.42(25),5120-5130(1999)
Kammasud, N., Boonyarat, C., Sanphanya, K., et al.5-Substituted pyrido[2,3-d]pyrimidine, an inhibitor against three receptor tyrosine kinasesBioorg. Med. Chem. Lett.19(3),745-750(2009)
Laird, A.D., Vajkoczy, P., Shawver, L.K., et al.SU6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumorsCancer Res.60(15),4152-4160(2000)
Griffin, R.J., Williams, B.W., Wild, R., et al.Simultaneous inhibition of the receptor kinase activity of vascular endothelial, fibroblast, and platelet-derived growth factors suppresses tumor growth and enhances tumor radiation responseCancer Res.62(6),1702-1706(2002)
Laird, A.D., Christensen, J.G., Li, G., et al.SU6668 inhibits Flk-1/KDR and PDGFRβ in vivo, resulting in rapid apoptosis of tumor vasculature and tumor regression in miceFASEB J.16(7),681-690(2002)
Gangjee, A., Kurup, S., Ihnat, M.A., et al.Synthesis and biological activity of N4-phenylsubstituted-6-(2,4-dichloro phenylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic and antitumor agentsBioorg. Med. Chem.18(10),3575-3587(2010)
Godl, K., Gruss, O.J., Eickhoff, J., et al.Proteomic characterization of the angiogenesis inhibitor SU6668 reveals multiple impacts on cellular kinase signalingCancer Res.65(15),6919-6926(2005)
Bain, J., Plater, L., Elliot, M., et al.The selectivity of protein kinase inhibitors: A further updateBiochem. J.408(3),297-315(2007)