Venadaparib, also known as IDX-1197, is a potent, selective and orally active PARP inhibitor with IC50s of 1 ~2 nM.. By inhibiting PARP, IDX-1197 stops cancer cells from repairing SSBs and drives the conversion of SSBs into double-strand breaks. IDX-1197 triggers a phenomenon known as synthetic lethality, which is defined by cell death resulting from the simultaneous perturbation of two genes without damaging normal cells. IDX-1197 is primarily aimed at treating homologous recombination deficient (HRD) patients. Notably, IDX-1197 has a particularly strong trapping effect, meaning it is more effective at trapping PARP1 and PARP2 enzymes on damaged DNA.
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名称 | Venadaparib |
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Iupac 化学名称 | 34-fluoro-7-aza-1(1)-phthalazina-5(1,3)-azetidina-3(1,3)-benzena-8(1)-cyclopropanaoctaphane-14(13H),4-dione |
同义词 | Venadaparib; IDX-1197; IDX 1197; IDX1197; |
英文同义词 | Venadaparib; IDX-1197; IDX 1197; IDX1197; |
分子式 | C23H23FN4O2 |
分子量 | 406.45 |
Smile | FC1=C(C(N2CC(CNC3CC3)C2)=O)C=C(C=C1)CC4=NNC(C5=C4C=CC=C5)=O |
InChiKey | YNBQAYKYNYRCCA-UHFFFAOYSA-N |
InChi | InChI=1S/C23H23FN4O2/c24-20-8-5-14(10-21-17-3-1-2-4-18(17)22(29)27-26-21)9-19(20)23(30)28-12-15(13-28)11-25-16-6-7-16/h1-5,8-9,15-16,25H,6-7,10-13H2,(H,27,29) |
Cas号 | 1681017-83-3 |
相关CAS号 |
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