Venadaparib(IDX-1197)

Catalog No.S9893 Batch:S989301

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Technical Data

Formula

C23H23FN4O2
Molecular Weight 406.45 CAS No. 1681017-83-3
Solubility (25°C)* In vitro DMSO 81 mg/mL (199.28 mM)
Ethanol 5 mg/mL (12.3 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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 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 treatment group.<sup><a class="sref" href="#s_ref">[1]</a></sup>

Protocol (from reference)

Animal Study:

[1]
  • Animal Models

    germline BRCA1-mutated ovarian cancer PDX model

  • Dosages

    -

  • Administration

    o.g.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.