ONX 0801 trisodium T38490

Product Introduction
Bioactivity


英文名: ONX 0801 trisodium

描述: ONX 0801 (BGC 945) trisodium is a targeted thymidylate synthase (TS) inhibitor specifically designed to act against tumors overexpressing the α-folate receptor.

体外活性: ONX 0801 (BGC 945) is designed to further reduce toxicity by more effectively targeting cancer cells that overexpress the α-FR[1]. ONX 0801 (BGC 945) exhibits IC 50 values of of 6.6 μM, 1.1 nM, 3.3 nM, 90 nM and 0.32 μM in A431, A431-FBP, KB, IGROV-1 and JEG-3 cells[2].

体内活性: BGC 945 (100 mg/kg, ip/iv injection) in the tumor had a longer half-life (28 hours) compared with other tissues[2]. BGC 945 (100 mg/kg daily for 16 days) does not lead to body weight loss, macroscopic signs of toxicity to the major organs, or a change in renal function[2]. BGC 945 at 100mg/kg induces a 5-20-fold increase in tumor dUrd at 4-72h without increases in the plasma, consistent with tumor targeting[2]. Animal Model: Mice (on the folate-free diet for 5 days were transplanted with tumor and the implants)[2]. Dosage: 100 mg/kg (Pharmacokinetic Analysis). Administration: Single i.p. or iv injection. Result: After i.p. injection, the compound was well absorbed from the peritoneal cavity. The plasma AUC was 50% higher for i.p. compared with i.v. administration and was also higher in spleen, kidney, and liver by this route. Tumor AUC was similar via either route.

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

关键字: BGC945 | BGC-945 | ONX 0801 trisodium | BGC 945 | ONX 0801 | ONX0801 | ONX-0801

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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