Nesuparib hydrochloride  (Synonyms: JPI-547/OCN-201 hydrochloride)

Nesuparib (JPI-547) hydrochloride 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 hydrochloride exhibits antitumor activity and can be used in research of advanced solid tumor^[1][2][3].

Nesuparib hydrochloride inhibits the activities of tankyrases, stabilizes AXIN protein, affects its downstream signaling pathways (WNT/β-catenin and Hippo signaling pathway), exhibiting antitumor effect^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Nesuparib hydrochloride exhibits antitumor activity against Olaparib (HY-10162)-resistant breast and ovary cancer in mouse BT474 or SNU251 xenograft models^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

473.40

C₂₃H₂₆Cl₂N₆O

2055357-65-6

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.