BT5528 is a bicyclic peptide toxin conjugate, an EphA2 activator. BT5528, made up of a bicyclic peptide and Auristatin E , is derivated from BCY6099. BT5528 shows potent anti-tumor activity without bleeding or coagulation toxicity in rats model In Vitro BT5528 shows high affinity on EphA2 with a K b value of 19.1 nM, and activates EphA2 in EphA2-expressing cells with an EC 50 value of 41.9 nM. BT5528 inhibits cancer cells growth with IC 50 s of 21.9 nM (HT-1080), 5.2 nM (PC-3), 21.6 nM (NCI-H1975), respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 . 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 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 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. Form:Solid IC50& Target:EC50: 41.9 nM (EphA2)
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BT5528
CAS number：2648849-70-9 molecular formula：C201H315N53O52S3
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 2648849-70-9 | molecular formula | C201H315N53O52S3 |
| molecular weight | 4403.14 g/mol | Exact mass | - |
| PSA | - | logp | - |
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