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Fluzoparib (SHR3162)

Cat. No. M10445
Fluzoparib (SHR3162) Structure
Synonym:

SHR3162; Fuzuopali; Fuzuloparibum

Size Price Availability Quantity
10mg USD 225  USD250 In stock
25mg USD 450  USD500 In stock
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Quality Control
  • Current batch:
  • Purity >98.5%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 472.40
Formula C22H16F4N6O2
CAS Number 1358715-18-0
Purity >98.5%
Solubility DMSO ≥ 50 mg/mL
Storage at -20°C
References

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.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Fluzoparib (SHR3162), SHR3162; Fuzuopali; Fuzuloparibum supplier, PARP, inhibitors

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