Identification | Back Directory | [Name]
Venadaparib | [CAS]
1681017-83-3 | [Synonyms]
IDX-1197 NOV140101 Venadaparib IDX-1197/Venadaparib Venadaparib(IDX-1197) inhibit,PARP,Venadaparib,IDX1197,Inhibitor,solid,IDX 1197,tumors,anticancer,poly ADP ribose polymerase 1(2H)-Phthalazinone, 4-[[3-[[3-[(cyclopropylamino)methyl]-1-azetidinyl]carbonyl]-4-fluorophenyl]methyl]- | [Molecular Formula]
C23H23FN4O2 | [MDL Number]
MFCD34470861 | [MOL File]
1681017-83-3.mol | [Molecular Weight]
406.45 |
Chemical Properties | Back Directory | [density ]
1.43±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 100 mg/mL (246.03 mM; Need ultrasonic) | [form ]
Solid | [pka]
12.06±0.40(Predicted) | [color ]
White to yellow |
Hazard Information | Back Directory | [Uses]
Venadaparib (IDX-1197) is a potent, selective and orally active PARP inhibitor with IC50s of 1.4 nM and 1.0 nM for PARP1 and PARP2, respectively. Venadaparib does not sensitive to PARP-5. Venadaparib prevents the repair of DNA single-strand breaks (SSB) and can be used for solid tumors research[1][2]. | [in vivo]
In the germline BRCA1-mutated ovarian cancer PDX model, oral administration of Venadaparib (IDX-1197) exhibits significant PAR inhibition (>90%) in tumor tissues until 24 hr post dose. Venadaparib also dose-dependently led to potent tumor growth inhibition compared to Olaparib treatment group[1]. | [IC 50]
PARP1: 1.4 nM (IC50); PARP2: 1 nM (IC50) | [References]
[1] Myongjae Lee, et al. Abstract A106: Development of IDX-1197, a novel, selective, and highly potent PARP inhibitor. American Association for Cancer Research, 2018. [2] Yong Man Kim, et al. First-in-human dose-finding study of venadaparib (IDX-1197), a potent and selective PARP inhibitor, in patients with advanced solid tumors. Journal of Clinical Oncology. 39, no. 15_suppl (May 20, 2021) 3107-3107. |
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InvivoChem
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13549236410 |
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https://www.invivochem.cn/ |
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guoyungurui
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18162595016; 18162595016 |
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