瑞卡帕布樟脑磺酸盐 T16807

Product Introduction
Bioactivity


英文名: Rucaparib monocamsylate

描述: Rucaparib monocamsylate (Rucaparib Camsylate) 是一种口服有效的 PARP 蛋白抑制剂，对 PARP-1 的Ki 为 1.4 nM。它是六磷酸己糖脱氢酶 (H6PD) 抑制剂，有用于去势抵抗性前列腺癌 (CRPC) 的研究潜力。

体外活性: Rucaparib is the most effective PARP inhibitor in enzyme assays (Ki: 1.4 nM). Rucaparib inhibits PARP-1 activity by 97.1% at a concentration of 1 μM in permeabilized D283Med cells. Rucaparib could target NF-κB activated by DNA damage and overcome toxicity observed with classical NF-κB inhibitors without compromising other vital inflammatory functions. The radio-sensitization by Rucaparib is due to downstream inhibition of activation of NF-κB and is independent of SSB repair inhibition [1][2][3].

体内活性: Rucaparib is not toxic but obviously enhances temozolomide-induced TGD in the DNA repair protein-competent D384Med xenografts. Rucaparib and AG14584 obviously (P < 0.05) increase temozolomide toxicity. Rucaparib enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts. Rucaparib significantly potentiates the cytotoxicity of topotecan and temozolomide in NB-1691, SH-SY-5Y, and SKNBE (2c) cells. Rucaparib (1 mg/kg) significantly increases temozolomide-induced body weight loss. Rucaparib (0.1 mg/kg) results in a 50% increase in the temozolomide-induced tumor growth delay. Pharmacokinetics studies also show that Rucaparib is detected in the brain tissue, which indicates that Rucaparib has potential in intra-cranial malignancy therapy [1][3][4].

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

溶解度: DMSO : 82.33 mg/mL(148.17 mM)


关键字: repair | H6PD | PARP | BRCA1 | poly ADP ribose polymerase | AG14644 | SSB | PF-01367338 monocamsylate | Capan-1 | Inhibitor | AG014699 monocamsylate | NF-κB | Rucaparib monocamsylate | inhibit | MX-1 | BRCA2

相关产品: Excisanin A | NU1025 | Buddlejasaponin IV | Lasiodin | Effusanin E | Paris saponin VII | YCH1899 | Furanodiene | Niraparib hydrochloride | VPC-70063

相关库: Drug Repurposing Compound Library | Anti-Prostate Cancer Compound Library | Anti-Cancer Drug Library | Clinical Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Anti-Cancer Active Compound Library | EMA Approved Drug Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途