| Bioactivity | Wortmannin-Rapamycin Conjugate 1 (compound 7c) is a furan ring-opened derivative of wortmannin-rapamycin conjugate with potent antitumor activities and a fine water solubility. Wortmannin-Rapamycin Conjugate 1 can inhibit the AKT phosphorylation in the tumor and can be used for cancer research[1]. |
| In Vivo | Wortmannin-Rapamycin Conjugate 1 (3,5 mg/kg, 静脉注射, 每周一次，13 d) 对 U87MG 小鼠异种移植模型具有显著的抗肿瘤活性[1]。Wortmannin-Rapamycin Conjugate 1 (15 mg/kg, 静脉注射, 2 h) 显著抑制 U87MG 小鼠异种移植模型肿瘤中 AKT 磷酸化[1]。Wortmannin-Rapamycin Conjugate 1 (15 mg/kg, 静脉注射, 每周一次，20 d ) 完全抑制荷瘤小鼠 HT29 结肠肿瘤的生长，HT29 是一种对雷帕霉素或沃特曼霉素类似物不敏感的结肠肿瘤模型[1]。Wortmannin-Rapamycin Conjugate 1 (30 mg/kg, 静脉注射, 每周一次，38 d ) 在 A498 荷瘤小鼠中与 200 μg 贝伐单抗 (HY-P9906) 联用，对较大的A498肿瘤有显著的消退作用[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| CAS | 1067892-47-0 |
| Formula | C88H131N3O23 |
| Molar Mass | 1598.99 |
| 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]. Ayral-Kaloustian S, et al. Hybrid inhibitors of phosphatidylinositol 3-kinase (PI3K) and the mammalian target of rapamycin (mTOR): design, synthesis, and superior antitumor activity of novel wortmannin-rapamycin conjugates. J Med Chem. 2010 Jan 14;53(1):452-9. |
Wortmannin-Rapamycin Conjugate 1
CAS: 1067892-47-0 F: C88H131N3O23 W: 1598.99
Wortmannin-Rapamycin Conjugate 1 (compound 7c) is a furan ring-opened derivative of wortmannin-rapamycin conjugate with
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