ONX 0801 (BGC 945) trisodium 是胸腺激酶合成酶(TS)的抑制剂，靶向α 叶酸受体过表达的肿瘤。
| 生物活性 | ONX 0801 (BGC 945) trisodium is athymidylate synthase(TS)inhibitor, targeted to α-folate receptor–overexpressing tumors[1][2]. |
体外研究
(In Vitro) | 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 IC50values 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].
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体内研究
(In Vivo) | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
