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ONX 0801 trisodium

ONX 0801 trisodium

产品编号 T38490   CAS 1097638-00-0
别名: Idetrexedtrisodium, BGC 945 trisodium, CB300945trisodium

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

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ONX 0801 trisodium Chemical Structure
ONX 0801 trisodium, CAS 1097638-00-0
规格 价格/CNY 货期 数量
25 mg ¥ 38,600 6-8周
药物设计专题培训
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
产品目录号及名称: ONX 0801 trisodium (T38490)
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参考文献
产品描述 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.
别名 Idetrexedtrisodium, BGC 945 trisodium, CB300945trisodium
分子量 716.61
分子式 C32H33N5Na3O10
CAS No. 1097638-00-0

存储

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

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TargetMol Library Books参考文献

1. Anna Tochowicz, et al. Development and binding mode assessment of N-[4-[2-propyn-1-yl[(6S)-4,6,7,8-tetrahydro-2-(hydroxymethyl)-4-oxo-3H-cyclopenta[g]quinazolin-6-yl]amino]benzoyl]-l-γ-glutamyl-D-glutamic acid (BGC 945), a novel thymidylate synthase inhibitor that targets tumor cells. J Med Chem. 2013 Jul 11;56(13):5446-55. 2. David D Gibbs, et al. BGC 945, a novel tumor-selective thymidylate synthase inhibitor targeted to alpha-folate receptor-overexpressing tumors. Cancer Res. 2005 Dec 15;65(24):11721-8. 3. Chau Ng, et al. Efficacy and tolerability of the thymidylate synthase (TS) inhibitor, BGC 945 is mediated through its selective uptake via the α-folate receptor (α-FR) in IGROV-1 human tumor xenografts. AACR Annual Meeting-- Apr 12-16, 2008; San Diego, CA.

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Keywords

ONX 0801 trisodium 1097638-00-0 BGC945 BGC-945 Idetrexedtrisodium BGC 945 trisodium BGC 945 ONX 0801 ONX0801 ONX-0801 CB300945trisodium Inhibitor inhibitor inhibit

 

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