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Venadaparib

Chemical Structure : Venadaparib

CAS No.: 1681017-83-3

Venadaparib (IDX-1197, IDX1197)

Catalog No.: PC-38102Not For Human Use, Lab Use Only.

Venadaparib (IDX-1197) is a potent, selective PARP inhibitor with IC50 of 1.4 nM and 1.0 nM for PARP1 and PARP2, respectively.

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Biological Activity

Venadaparib (IDX-1197) is a potent, selective PARP inhibitor with IC50 of 1.4 nM and 1.0 nM for PARP1 and PARP2, respectively.
IDX-1197 does not inhibits PARP5A (Tankyrase-1, IC50>10 uM), which belongs to the PARP family.
IDX-1197 significantly inhibited PARP1-mediated PAR expression in DNA damage-induced Hela cells.
IDX-1197 exhibits potent tumor growth inhibition in germline BRCA1-mutated ovarian cancer PDX model.
IDX-1197 shows improved antitumor activity against breast cancer PDX models, which included both germline BRCA-mutated and non-germline BRCA-mutated models, compared with olaparib and/or niraparib.

Physicochemical Properties

M.Wt 406.461
Formula C23H23FN4O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-(3-(3-((cyclopropylamino)methyl)azetidine-1-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one

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.

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