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Cat. No.: HY-145584A

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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.

For research use only. We do not sell to patients.

CAS No.: 2055357-65-6
Formula: C₂₃H₂₆Cl₂N₆O
Molecular Weight:473.40

Storage:

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

Nesuparib hydrochloride Chemical Structure

CAS No.: 2055357-65-6

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[2]

PARP2

2 nM (IC₅₀)

tankyrase-2

1 nM (IC₅₀)

tankyrase-1

5 nM (IC₅₀)

All PARP Isoforms :

All Wnt Isoforms :

In Vitro

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.

In Vivo

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.

Chemical Information

CAS No. 2055357-65-6
Molecular Weight 473.40
Formula C₂₃H₂₆Cl₂N₆O
SMILES

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

JPI-547/OCN-201 hydrochloride
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[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.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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Nesuparib hydrochloride

All PARP Isoforms

All Wnt Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

Nesuparib hydrochloride Related Classifications

HY-145584A Related Classifications