Venadaparib hydrochloride

Names

[ Name ]:
Venadaparib hydrochloride

Biological Activity

[Description]:

Venadaparib (IDX-1197) hydrochloride is a potent and selective PARP inhibitor with anticancer activities. Venadaparib hydrochloride can be used for solid tumors research[1][2].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> PARP

Signaling Pathways >> Cell Cycle/DNA Damage >> PARP

[Target]

PARP1:1.4 nM (IC50)

PARP2:1 nM (IC50)

[In Vitro]

Venadaparib (example 143; 6-10 days) shows potent growth inhibition of MDA-MB-436 cells and Capan-1 pancreatic cancer cells with IC50 values of ≤5nM and 50nM [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].

[References]

[1]. 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.

[2]. Jae-Hoon Kang, et al. A novel phtalazinone derivatives and manufacturing process thereof. WO2015037939A1.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₃H₂₄ClFN₄O₂

[ Molecular Weight ]:
442.91

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.