Fuzuopali
| CAS号 | 1358715-18-0 | 货号 | BCP38585 |
| 中文名 | Fuzuopali | ||
| 英文名 | Fuzuopali | ||
| 中文别名 | |||
| 英文别名 | SHR-3162;SHR 3162;SHR3162; | ||
| 分子式 | C22H16F4N6O2 | 分子量 | 472.4 |
| 生物活性 | Fluzoparib is a selective poly [ADP-ribose] polymerase 1 (PARP1) and poly [ADP-ribose] polymerase 2 inhibitor (PARP2), being developed by Jiangsu HengRui Medicine, for the treatment of cancer. PARP enzymes play a vital role in repair of DNA damage and maintaining genomic stability. Fluzoparib inhibits PARP enzymes and induces DNA-double strands breaks, G2/M arrest and apoptosis in homologous recombination repair (HR)-deficient cells. Clinical development for ovarian cancer, breast cancer, fallopian tube cancer, peritoneal cancer, gastric cancer and solid tumours is underway in China and Australia. An orally available inhibitor of poly (ADP-ribose) polymerase (PARP) types 1 and 2, with potential antineoplastic activity. Upon oral administration, fluzoparib inhibits PARP 1 and 2 activity, which inhibits PARP-mediated repair of damaged DNA via the base excision repair (BER) pathway, enhances the accumulation of DNA strand breaks, promotes genomic instability, and leads to an induction of apoptosis. The PARP family of proteins catalyze post-translational ADP-ribosylation of nuclear proteins, which then transduce signals to recruit other proteins to repair damaged DNA. PARP inhibition may enhance the cytotoxicity of DNA-damaging agents and may reverse tumor cell chemoresistance and radioresistance. | ||
| 信号通路 | Cell Cycle/DNA Damage Epigenetics | ||
| 靶 点 | PARP | ||
结构式
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