Home DNA Damage/DNA Repair PARP inhibitor Venadaparib(IDX-1197) For research use only.

Venadaparib(IDX-1197)

Venadaparib (IDX-1197), a potent PARP1/2 inhibitor with IC50 values of 1.4 nM and 1.0 nM respectively, prevents the repair of DNA single-strand breaks (SSB) and promotes the conversion of SSB to double-stranded breaks (DSB), which ultimately leads to synthetic lethality in cancer cells.

Venadaparib(IDX-1197) Chemical Structure

Venadaparib(IDX-1197) Chemical Structure

CAS: 1681017-83-3

Purity & Quality Control

Batch: S989301 DMSO] 81 mg/mL] false] Ethanol] 5 mg/mL] false] Water] Insoluble] false Purity: 99.76%
99.76

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Signaling Pathway

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PARP Signaling Pathway

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Biological Activity

Description Venadaparib (IDX-1197), a potent PARP1/2 inhibitor with IC50 values of 1.4 nM and 1.0 nM respectively, prevents the repair of DNA single-strand breaks (SSB) and promotes the conversion of SSB to double-stranded breaks (DSB), which ultimately leads to synthetic lethality in cancer cells.
Targets
PARP2 [1]
(in enzyme assay)		 PARP1 [1]
(in enzyme assay)
1 nM 1.4 nM
In vitro
In vitro

IDX-1197 potently, selectively inhibits PARP1 and PARP2 activities with no sensitivity to PARP5A (Tankyrase-1), and significantly inhibits PARP1-mediated PAR expression in DNA damage-induced Hela cells.<sup><a class="sref" href="#s_ref">[1]</a></sup>
In Vivo
In vivo

In the germline BRCA1-mutated ovarian cancer PDX model, oral administration of IDX-1197 exhibits significant PAR inhibition in tumor tissues, and dose-dependently lead to potent tumor growth inhibition compared to Olaparib treatment group.<sup><a class="sref" href="#s_ref">[1]</a></sup>
Animal Research Animal Models germline BRCA1-mutated ovarian cancer PDX model
Dosages -
Administration o.g.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05202912 Completed
Healthy Male
Idience Co. Ltd.
 January 16 2022 Phase 1

Chemical Information & Solubility

Molecular Weight 406.45 Formula

C23H23FN4O2
CAS No. 1681017-83-3 SDF --
Smiles FC1=C(C=C(CC2=NNC(=O)C3=CC=CC=C23)C=C1)C(=O)N4CC(CNC5CC5)C4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 81 mg/mL ( (199.28 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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