Description
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.
Product information
CAS Number: 1681017-83-3
Molecular Weight: 406.45
Formula: C23H23FN4O2
Chemical Name: 4-[(3-{3-[(cyclopropylamino)methyl]azetidine-1-carbonyl}-4-fluorophenyl)methyl]-1,2-dihydrophthalazin-1-one
Smiles: O=C1NN=C(CC2=CC(=C(F)C=C2)C(=O)N2CC(CNC3CC3)C2)C2=CC=CC=C12
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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 100 mg/mL (246.03 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
In DNA damage-induced Hela cells, Venadaparib (IDX-1197) significantly inhibits PARP1-mediated PAR expression (EC50 of 0.5 nM).
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.
Products are for research use only. Not for human use.
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