Fluzoparib

SKU: orb1298619

Description

Fluzoparib (SHR3162) is an oral PARP inhibitor developed for cancer research. It demonstrates potent activity in vitro and has shown antitumor efficacy in vivo models of solid tumors, supporting its investigation for oncology applications.

Research Area

Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 1358715-18-0
• MW: 472.4
• Purity: 99.63% (May vary between batches)
• Formula: C₂₂H₁₆F₄N₆O₂
• SMILES: Fc1ccc(Cc2n[nH]c(=O)c3ccccc23)cc1C(=O)N1CCn2nc(nc2C1)C(F)(F)F
• Target: PARP
• Solubility: DMSO:88.33 mg/mL (186.98 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.99 mM)

Bioactivity

• Target IC50:
  PARP1:1.46±0.72 nM (IC50)
• In Vivo:
  In vitro experiments in NSCLC cell lines along with in vivo experiments using an NSCLC xenograft mouse model demonstrated the radiosensitization effect of fluzoparib. The underlying mechanisms involved increased apoptosis, cell-cycle arrest, enhanced irradiation-induced DNA damage, and delayed DNA-damage repair.
• In Vitro:
  Fluzoparib potently inhibited PARP1 enzyme activity and induced DNA double-strand breaks, G2 /M arrest, and apoptosis in homologous recombination repair (HR)-deficient cells. Fluzoparib preferentially inhibited the proliferation of HR-deficient cells and sensitized both HR-deficient and HR-proficient cells to cytotoxic drugs. Notably, fluzoparib showed good pharmacokinetic properties, favorable toxicity profile, and superior antitumor activity in HR-deficient xenografts models. Furthermore, fluzoparib in combination with apatinib or with apatinib plus paclitaxel elicited significantly improved antitumor responses without extra toxicity.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

cancer, inhibit, Inhibitor, PARP1, PARP, Fluzoparib, Fuzuloparib, homologous recombination repair, HS 10160, HS10160, HS-10160, ovarian, poly ADP ribose polymerase, SHR 3162, SHR3162, SHR-3162

Compound Identifiers

PubChem CID

56649297