Nesuparib free base

Nesuparib is the orally active inhibitor.

For research use only. Not for human or veterinary use.

Target PARP Wnt β-catenin

Research area Neurological Disease Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

Nesuparib structure

CAS No.: 2055357-64-5

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
50 mg	USD 480.00	BP-02155-50mg	In stock	Get quote
100 mg	USD 750.00	BP-02155-100mg	In stock	Get quote
250 mg	USD 1,450.00	BP-02155-250mg	In stock	Get quote
500 mg	USD 2,280.00	BP-02155-500mg	In stock	Get quote
1 g	USD 3,600.00	BP-02155-1g	In stock	Get quote

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Description

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.

Biological activity

In Vitro Nesuparib inhibits the activities of tankyrases, stabilizes AXIN protein, affects its downstream signaling pathways (WNT/β-catenin and Hippo signaling pathway), exhibiting antitumor effect. In Vivo Nesuparib exhibits antitumor activity against Olaparib (HY-10162)-resistant breast and ovary cancer in mouse BT474 or SNU251 xenograft models.

Identifiers

SMILES: N#CC1=CN=C(N2CCN(CC2)CC3=CC(NC(C4=C5NCCC4)=O)=C5C=C3)C=C1
InChIKey: GRPXLKXGJAGYSD-UHFFFAOYSA-N

Specifications

MW (average): 400.4763
Formula: C₂₃H₂₄N₆O
CAS No.: 2055357-64-5
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C 3 years, 4°C 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO 60 mg/mL

Documents

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.

Same target

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Same research area

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