Nesuparib

Nesuparib (JPI-547) is the orally active inhibitor for PARP 1/2 and Tankyrase 1/2 that inhibits tankyrases 1, tankyrases 2, and PARP 1 with IC50s of 5, 1 and 2 nM, respectively. Nesuparib exhibits antitumor activity and can be used in research of advanced solid tumor[1][2][3].

Product Specifications

CAS Number

[2055357-64-5]

Product Name Alternative

JPI-547/OCN-201

UNSPSC

12352005

Target

PARP; Wnt; β-catenin

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics; Stem Cell/Wnt

Applications

Neuroscience-Neurodegeneration

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/nesuparib.html

Purity

99.54

Solubility

DMSO : 60 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

N#CC1=CN=C(N2CCN(CC2)CC3=CC(NC(C4=C5NCCC4)=O)=C5C=C3)C=C1

Molecular Formula

C23H24N6O

Molecular Weight

400.48

References & Citations

[1]Tricyclic derivative compound, method for preparing same, and pharmaceutical composition comprising same. Patent WO2016200101A2.|[2]Im S A , et al.A phase I dose-escalation and expansion study of JPI-547, a dual inhibitor of PARP/tankyrase in patients with advanced solid tumors.[J].Journal of Clinical Oncology, 2021, 39 (15_suppl) :3113-3113.|[3]Oh K S, et al. JPI-547, a dual inhibitor of PARP/Tankyrase, shows promising antitumor activity against pancreatic cancers with homologous recombination repair deficiency or Wnt-addiction[J]. Cancer Research, 2023, 83 (7_Supplement) : 4496-4496.