Fluzoparib

Fluzoparib (SHR3162) is a potent and orally active PARP1 inhibitor (IC50=1.46±0.72 nM, a cell-free enzymatic assay) with superior antitumor activity. Fluzoparib selectively inhibits the proliferation of homologous recombination repair (HR) -deficient cells, and sensitizes both HR-deficient and HR-proficient cells to cytotoxic agents. Fluzoparib exhibits good pharmacokinetic properties in vivo and can be used for BRCA1/2-mutant relapsed ovarian cancer research[1].

Product Specifications

CAS Number

[1358715-18-0]

Product Name Alternative

SHR3162; Fuzuloparib

UNSPSC

12352005

Hazard Statement

H302, H315, H319

Target

PARP

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

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

Purity

99.96

Solubility

DMSO : 33.33 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C1NN=C(CC2=CC=C(F)C(C(N3CC4=NC(C(F)(F)F)=NN4CC3)=O)=C2)C5=C1C=CC=C5

Molecular Formula

C22H16F4N6O2

Molecular Weight

472.40

Precautions

H302, H315, H319

References & Citations

[1]Lei Wang, et al. Pharmacologic characterization of fluzoparib, a novel poly (ADP-ribose) polymerase inhibitor undergoing clinical trials. Cancer Sci. 2019 Mar;110 (3) :1064-1075.|[2]Huiping Li, et al. Phase I dose-escalation and expansion study of PARP inhibitor, fluzoparib (SHR3162), in patients with advanced solid tumors. Chin J Cancer Res. 2020 Jun;32 (3) :370-382.