Product Introduction
Bioactivity


英文名: Fluzoparib

描述: Fluzoparib (SHR3162) 是口服活性 PARP1抑制剂，IC50为1.46±0.72  nM，在体内具有良好的药代动力学特性，具有抗肿瘤活性，可用于癌症研究。它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。

体外活性: 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.

体内活性: 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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 94 mg/mL (198.98 mM)


关键字: homologous recombination repair | Inhibitor | poly ADP ribose polymerase | inhibit | ovarian | SHR-3162 | Fluzoparib | PARP | PARP1 | HS 10160 | HS-10160 | Fuzuloparib | cancer | SHR 3162

相关产品: Dehydrocorydaline | 1-[2,4-Dihydroxy-6-methoxy-3-(3-methyl-2-buten-1-yl)phenyl]-3-(4-hydroxyphenyl)-2-propen-1-one | ME0328 | WAY-620473 | BYK204165 | VPC-70063 | Britannilactone diacetate | Cearoin | Glycoborinine | 4-amino-1,8-Naphthalimide

相关库: Drug Repurposing Compound Library | Anti-Prostate Cancer Compound Library | Approved Drug Library | FDA-Approved & Pharmacopeia Drug Library | Anti-Cancer Compound Library | NMPA-Approved Drug Library | Anti-Cancer Approved Drug Library | Orally Active Compound Library | NO PAINS Compound Library