Fuzuopali is a poly (ADP-ribose) polymerase inhibitor (PARP) inhibitor with IC50 of 1.46±0.72 nM for 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 acts synergistically to inhibit cell growth and promote apoptosis among lung cancer cells.
In vivo, Fluzoparib (30 mg/kg; oral gavage; 21 days) apparently inhibits the growth of tumor with an inhibition rate of 59% (day 21) at 30 mg/kg, and it does not cause significant loss of body weight in Nude mice bearing MDA‐MB‐436 (BRCA1‐deficient) model.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO ≥ 50 mg/mL|
Phase I dose-escalation and expansion study of PARP inhibitor, fluzoparib (SHR3162), in patients with advanced solid tumors.
Huiping Li, et al. Chin J Cancer Res. 2020 Jun;32(3):370-382. PMID: 32694901.
Pharmacologic characterization of fluzoparib, a novel poly(ADP-ribose) polymerase inhibitor undergoing clinical trials.
Lei Wang, et al. Cancer Sci. 2019 Mar;110(3):1064-1075. PMID: 30663191.
|Related PARP Products|
AZD5305 is a potent and oral active, second-generation PARP (highly selective PARP1) inhibitor.
BRCA1-IN-2 is a cell-permeable protein-protein interaction (PPI) inhibitor for BRCA1, with IC50 of 0.31 μM and Kd of 0.3 μM.
RBN-2397 is a potent and orally active NAD+ competitive inhibitor of PARP7 (IC50<3 nM).
Pamiparib (BGB-290) is an orally active, potent, highly selective inhibitor of PARP1 and PARP2 with IC50 values of 0.9 nM and 0.5 nM, respectively.
BGP-15 is a novel poly(ADP-ribose) polymerase inhibitor with an IC50 and a Ki of 120 μM and 57 μM, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.