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Fluzoparib

CAS No. : 1358715-18-0

MCE 站：Fluzoparib

产品活性：Fluzoparib (SHR3162) 是一种有效的口服活性 PARP1 抑制剂(IC₅₀=1.46±0.72? nM)，具有优越的抗肿瘤活性。Fluzoparib 选择性地抑制同源重组修复 (HR) 缺陷细胞的增殖，并使 HR 缺陷细胞对细胞毒性药物敏感。Fluzoparib 在体内具有良好的药代动力学特性，可用于癌症研究。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics

作用靶点：PARP

In Vitro: Fluzoparib (30?μM; 24 hour) increases the levels of γH2AX in a concentration‐dependent manner in both?BRCA2‐deficient V‐C8 cells and?BRCA1‐deficient MDA‐MB‐436 cells, but not in?BRCA‐proficient V‐C8#13‐5 cells.
Fluzoparib (10?μM; 24 hour) increases levels of both pCDK1 and cyclin B, indicating activation of the G2/M checkpoint in MDA‐MB‐436 cells.
Fluzoparib (10?μM; 72 hour) increases the processing of caspase‐3, ‐8, and ‐9 concentration‐dependently, it induces G2/M arrest and apoptosis in HR‐deficient?MDA‐MB‐436 cells?cells.
Fluzoparib is preferentially efficacious against HR‐deficient cells, such as BRCA1‐deficient (UWB1.289), MDA‐MB‐436, BRCA2‐deficient (V‐C8), BRCA1‐deficientBRCA2‐mutated (MX‐1) and BRCA1?hypermethylated (OVCAR‐8) cells with IC₅₀ values of 0.51?μM, 1.57?μM, 0.053?μM, 1.57?μM, and 1.43?μM, respectively. The IC₅₀ values for HR‐proficient cells (V‐C8#13‐5 and UWB1.289 BRCA1) are both >10?μM.

In Vivo: Fluzoparib (oral gavage; 0.3, 1, or 3?mg/kg; single dose) exhibits a good pharmacokinetic profile in Female Balb/cA nude mice (5‐6 weeks old) mice bearing MDA‐MB‐436. After a single oral dose, fluzoparib is rapidly absorbed and rapidly cleared from blood at all dose levels; plasma concentrations of fluzoparib quickly reaches maximum within 2?hours. In contrast, concentrations of fluzoparib in tumor remains at high levels even at 24?hours after dosing (57.9?ng/g , 39.3 ng/g, and 85.6?ng/g for doses of 0.3, 1, and 3?mg/kg, respectively).
Fluzoparib (oral gavage; 30 mg/kg; 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.
Fluzoparib (3mg/kg) combines with Cisplatin, Paclitaxel, or Apatinib (oral gavage; BID; 21 days) causes growth inhibition with rates of 61.4%, 55.3%, and 72.8%, respectively.
Fluzoparib, Cisplatin, and Apatinib combination or Fluzoparib, Paclitaxel, and Apatinib combination can cause growth inhibition with rates of 84.9% and 75.6% (day 21), respectively in vivo.
The 2‐drug combination of Fluzoparib with cisplatin and The 3‐drug Fluzoparib, Cisplatin, and Apatinib combination lead to loss of body weight, whereas no apparent toxicity was observed in other combinations.

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