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  3. HIT218852161
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HIT218852161
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HIT218852161
  • HIT ID:HIT218852161
  • Cas No:2889316-21-4
  • 常用名:DBPR112 HCl
  • IUPAC:(2E)-4-(dimethylamino)-N-[3-(4-{[(1S)-2-hydroxy-1-phenylethyl]amino}-6-phenylfuro[2,3-d]pyrimidin-5-yl)phenyl]but-2-enamide hydrochloride
    IUPAC:(2E)-4-(dimethylamino)-N-[3-(4-{[(1S)-2-hydroxy-1-phenylethyl]amino}-6-phenylfuro[2,3-d]pyrimidin-5-yl)phenyl]but-2-enamide hydrochloride
  • InChI key:ZFZWVQVZJNHGDO-NJCJUFJCSA-N
  • 分子式:C32H32ClN5O3
  • 分子量:570.09
  • 氢键供体数 (HBD):
  • 氢键受体数 (HBA):
  • LogP:
  • SMILES:Cl.CN(C)C\C=C\C(=O)Nc1cccc(c1)-c1c(oc2ncnc(N[C@H](CO)c3ccccc3)c12)-c1ccccc1
    SMILES:Cl.CN(C)C\C=C\C(=O)Nc1cccc(c1)-c1c(oc2ncnc(N[C@H](CO)c3ccccc3)c12)-c1ccccc1
  • DBPR112 is a potent EGFR inhibitor (IC50=487 nM) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. DBPR112), DBPR112<br/><br/>not only displayed a potent inhibitory activity against EGFRL858R/T790M double mutations but also exhibited tenfold potency better than the third-generation inhibitor, osimertinib,against EGFR and HER2 exon 20 insertion mutations. Overall, pharmacokinetic improvement through lead-to-candidate<br/><br/>optimization yielded fourfold oral AUC better that afatinib along with F = 41.5%, an encouraging safety profile, and significant antitumor efficacy in in vivo xenograft models.
市场产品/服务共显示1个结果
  • 供应商
    TargetMolSC
    规格
    货期
    1-2周
    纯度
    -
    ¥ 11,700.00
    1

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