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HIT220913803
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HIT220913803
  • HIT ID:HIT220913803
  • Cas No:
  • 常用名:AG-012986
  • IUPAC:4-{[4-amino-5-(2,6-difluorobenzoyl)-1,3-thiazol-2-yl]amino}-N-[(2R)-1-(dimethylamino)propan-2-yl]benzamide
    IUPAC:4-{[4-amino-5-(2,6-difluorobenzoyl)-1,3-thiazol-2-yl]amino}-N-[(2R)-1-(dimethylamino)propan-2-yl]benzamide
  • InChI key:InChIKey=KFWFBALDPSVAFT-GFCCVEGCSA-N
  • 分子式:C22H23F2N5O2S
  • 分子量:459.52
  • 氢键供体数 (HBD):
  • 氢键受体数 (HBA):
  • LogP:
  • SMILES:C[C@H](CN(C)C)NC(=O)c1ccc(Nc2nc(N)c(s2)C(=O)c2c(F)cccc2F)cc1
    SMILES:C[C@H](CN(C)C)NC(=O)c1ccc(Nc2nc(N)c(s2)C(=O)c2c(F)cccc2F)cc1
  • AG-012986 is a multitargeted cyclin-dependent kinase (CDK) inhibitor active against CDK1, CDK2, CDK4/6, CDK5, and CDK9, with selectivity over a diverse panel of non-CDK kinases. AG-012986 showed antiproliferative activities in vitro with IC(50)s of <100 nmol/L in 14 of 18 tumor cell lines. In vivo, significant antitumor efficacy induced by AG-012986 was seen (tumor growth inhibition, >83.1%) in 10 of 11 human xenograft tumor models. AG-012986 also showed dose-dependent retinoblastoma Ser(795) hypophosphorylation, cell cycle arrest, decreased Ki-67 tumor staining, and apoptosis in conjunction with antitumor activity.
市场产品/服务共显示1个结果
  • 供应商
    TargetMolSC
    规格
    货期
    6-8周
    纯度
    -
    ¥ 10,600.00
    1

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