| Bioactivity | BGC0222 is a novel prodrug of Irinotecan (HY-16562). BGC0222, as a PEG-cRGD-conjugated Irinotecan (HY-16562) derivative, could slowly and steadily release Irinotecan (HY-16562). BGC0222 binds to αVβ3 with IC50 values of 4.25 μM (αVβ3) and 58.7 μM (αVβ5). BGC0222 possesses the property of inducing neovascularization. BGC0222 exhibits good antiproliferation activity in many tumors[1]. |
| Invitro | BGC0222 (72 h) 与 Irinotecan (HY-16562) 和 NKTR-102 相比，对 HT29、MIA PaCa-2 和 MCF-7 肿瘤细胞具有更好的抗增殖活性，IC50 分别为 1.83 μM、3.95 μM 和 0.68 μM[1]。BGC0222 (40 μM) 显示出良好的血管生成活性，血管长度达 1930 mm (CAM 血管生成试验)[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> BGC0222 相关抗体: |
| In Vivo | BGC0222 (20-60 mg/kg，静脉注射，每 4 天或每周 1 次，共 3 次) 在 HT-29、MIA PaCa-2、NCI-H446、U-87 MG 和 MDA-MB-231 异种移植裸鼠中表现出显著的抗增殖活性，其 RTV 和 T/C 值均低于 Irinotecan[1]。BGC0222 (30-90 mg/kg，静脉注射，每周一次，为期 28 天) 在 Sprague-Dawley 大鼠体内的安全性irinotecan 相比有所改善，最大耐受剂量 (MTD) 分别为 90 mg/kg和低于 60 mg/kg[1]。BGC0222 (20-80 mg/kg，静脉注射，单次) 在 Sprague-Dawley 大鼠体内缓慢而稳定地释放Irinotecan[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| Formula | C1241H2276N64O552 |
| Molar Mass | 26927.36 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Huang YQ, et al. Design, synthesis and pharmacological evaluation of a novel PEG-cRGD-conjugated irinotecan derivative as potential antitumor agent. Eur J Med Chem. 2018 Oct 5, 158:82-90. |