跳转到内容

利尼伐尼

维基百科,自由的百科全书
利尼伐尼
臨床資料
ATC碼
  • 未分配
法律規範狀態
法律規範
识别信息
  • 1-[4-(3-amino-1H-indazol-4-yl)phenyl]-3-(2-fluoro-5-methylphenyl)urea
CAS号796967-16-3
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.206.772 編輯維基數據鏈接
化学信息
化学式C17H15FN5O
摩尔质量324.34 g·mol−1
3D模型(JSmol英语JSmol
  • Cc1ccc(F)c(NC(=O)Nc2ccc(-c3cccc4[nH]nc(N)c34)cc2)c1
  • InChI=1S/C21H18FN5O/c1-12-5-10-16(22)18(11-12)25-21(28)24-14-8-6-13(7-9-14)15-3-2-4-17-19(15)20(23)27-26-17/h2-11H,1H3,(H3,23,26,27)(H2,24,25,28)
  • Key:MPVGZUGXCQEXTM-UHFFFAOYSA-N

利尼伐尼(英語:Linifanib,研发代号:ABT-869)是一种结构新颖、强效的受體酪氨酸激酶(RTK)、血管内皮生长因子(VEGF)和血小板衍生生長因子(PDGF)抑制剂,对人内皮细胞血小板衍生生长因子受体β英语PDGFRB(PDGFR-β)、激酶插入域受体英语Kinase insert domain receptor(KDR)和集落刺激因子1受体英语Colony stimulating factor 1 receptor(CSF-1R)的IC50分别为0.2,2,4和7nM。它对不相关的RTK、可溶性酪氨酸激酶或丝氨酸/苏氨酸激酶英语Serine/threonine-specific protein kinase的活性较低(IC50>1μM)。口服的利尼伐尼在机制导向的VEGF诱发的子宫水肿ED-50英语Effective_dose_(pharmacology)#ED50=0.5mg/kg)和角膜血管新生(>50%抑制,15 mg/kg)的体内实验小鼠模型中显示有效[1][2]

该物质已被用作化学品混合液的一部分,以将衰老的人类细胞变回年轻细胞(以转录组年龄衡量),而不将它们完全变成未分化的诱导性多能干细胞[3]

参考来源

[编辑]
  1. ^ Albert DH, Tapang P, Magoc TJ, Pease LJ, Reuter DR, Wei RQ, Li J, Guo J, Bousquet PF, Ghoreishi-Haack NS, Wang B, Bukofzer GT, Wang YC, Stavropoulos JA, Hartandi K, Niquette AL, Soni N, Johnson EF, McCall JO, Bouska JJ, Luo Y, Donawho CK, Dai Y, Marcotte PA, Glaser KB, Michaelides MR, Davidsen SK. Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor. Molecular Cancer Therapeutics. 2006-04, 5 (4): 995–1006. PMID 16648571. doi:10.1158/1535-7163.MCT-05-0410. 
  2. ^ Guo J, Marcotte PA, McCall JO, Dai Y, Pease LJ, Michaelides MR, Davidsen SK, Glaser KB. Inhibition of phosphorylation of the colony-stimulating factor-1 receptor (c-Fms) tyrosine kinase in transfected cells by ABT-869 and other tyrosine kinase inhibitors. Molecular Cancer Therapeutics. 2006-04, 5 (4): 1007–1013. PMID 16648572. doi:10.1158/1535-7163.MCT-05-0359可免费查阅. 
  3. ^ Yang JH, Petty CA, Dixon-McDougall T, Lopez MV, Tyshkovskiy A, Maybury-Lewis S, Tian X, Ibrahim N, Chen Z, Griffin PT, Arnold M, Li J, Martinez OA, Behn A, Rogers-Hammond R, Angeli S, Gladyshev VN, Sinclair DA. Chemically induced reprogramming to reverse cellular aging. Aging. 2023-07, 15 (13): 5966–5989. PMC 10373966可免费查阅. PMID 37437248. doi:10.18632/aging.204896.