BT5528 是一种双环肽毒素结合物，一种EphA2激活剂。BT5528 由双环肽和 Auristatin E (HY-15582) 组成，是 BCY6099 的衍生物。BT5528 在大鼠模型中显示出强大的抗肿瘤活性，不导致出血或引起凝血毒性。
| 生物活性 | BT5528 is a bicyclic peptide toxin conjugate, anEphA2activator. BT5528, made up of a bicyclic peptide andAuristatinE(HY-15582), is derivated from BCY6099. BT5528 shows potent anti-tumor activity without bleeding or coagulation toxicity in rats model[1][2]. |
| IC50& Target | |
体外研究
(In Vitro) | BT5528 shows high affinity on EphA2 with a Kbvalue of 19.1 nM, and activates EphA2 in EphA2-expressing cells with an EC50value of 41.9 nM[1].
BT5528 inhibits cancer cells growth with IC50s of 21.9 nM (HT-1080), 5.2 nM (PC-3), 21.6 nM (NCI-H1975), respectively[1].
|
体内研究
(In Vivo) | BT5528 (1, 2, 3 mg/kg; i.v.; once a week; 2-5 weeks) inhibits tumor growth in vivo in mice xenograft model[1].
BT5528 (3 mg/kg; i.v.; once a week; 3 weeks) exhibits greate ability to penetrate solid tumours in Non-small-cell lung carcinoma (NSCLC) Patient-derived xenograft (PDX) xenograft model in mice[1].
| Animal Model: | Xenograft model in mice with NCI-H1975 Non-small cell lung cancer, MDA-MB-231 Triple-negative breast cancer, MOLP-8 Multiple Myeloma[1] | | Dosage: | 1, 2, 3 mg/kg | | Administration: | Intravenous injection; once a week; for 5, 3, 2 weeks respectively | | Result: | Showed target-mediated efficacy in the high EphA2-expressing NCI-H1975 NSCLC xenograft and MDA-MB-231 TNBC xenograft, but there were no significant effects in the low EphA2-expressing MOLP-8 Multiple Myeloma xenograft. |
| Animal Model: | Non-small-cell lung carcinoma (NSCLC) Patient-derived xenograft (PDX) xenograft model in mice[1] | | Dosage: | 3 mg/kg; compared with MEDI 547 (3 mg/kg) | | Administration: | Intravenous injection; once a week; for 3-4 weeks | | Result: | Maintained efficacy during 3 weeks, while MEDI-547 fails to show efficacy.
Didn’t affect D-Dimer, APTT or liver enzyme parameters. |
|
| Clinical Trial | |
| 分子量 | |
| Formula | |
| CAS 号 | |
| 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. |
m.cnreagent.com