BT7480_product_DataBase

Bioactivity	BT7480 (BCY11863) is one of the Bicycle tumor-targeted immune cell agonists (Bicycle TICAs). BT7480 is an angonist of CD137 (4-1BB). BT7480 consists of a poly(ethylene glycol) (PEG)-based linker, and a synthetic Bicycle peptide targeting CD137 conjugated to Bicycles targeting Nectin-4. Nectin-4 is a cell adhesion molecule, overexpressing in multiple tumor cells. BT7480 elicits significant CD137 agonism and potent antitumor activity in syngeneic mouse models[1][2].
Target	CD137 (4-1BB)
Invitro	BT7480 导致原代人免疫细胞中促炎细胞因子 IFNγ 和 IL-2 的分泌呈剂量依赖性增加 (EC50=0.22 nM 和 0.36 nM)，而 HT1376 肿瘤细胞与来自健康供体的人外周血单核细胞 (PBMC) 共培养并用抗 CD3 处理以刺激 CD137 在免疫细胞上的表达[1]。
In Vivo	BT7480（5 mg/kg；腹腔注射；每天一次，持续 10 天）在 CT26-Nectin-4/huCD137 小鼠模型中表现出抗肿瘤活性[1]。BT7480（2 mg/kg；静脉注射；单剂量）的 CL 为 8.5 mL/min/kg，终末半衰期为 3.6 小时[1]。BT7480（1、5、10 和 30 mg/kg；腹腔注射；单剂量）导致 CD-1 小鼠的暴露量 (AUCinf) 剂量依赖性增加[1] 。BT7480（1 和 10 mg/kg；腹腔注射；每天 3 次，持续 40 天）在小鼠 MC38-Nectin-4 肿瘤模型中导致肿瘤消退[1]。在食蟹猴 MC38 同基因模型中的药代动力学分析[1]Route
Name	BT7480
CAS	2762739-36-4
Formula	C331H467N73O89S10
Molar Mass	7213.34
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]. Upadhyaya P, et al. Discovery and Optimization of a Synthetic Class of Nectin-4-Targeted CD137 Agonists for Immuno-oncology. J Med Chem. 2022 Jul 28;65(14):9858-9872. [2]. Hurov K, et al. A novel fully synthetic dual targeted Nectin-4/4-1BB Bicycle (R) peptide induces tumor localized 4-1BB agonism[J]. J. Immunother. Cancer, 2019, 7.

PeptideDB

BT7480

CAS: 2762739-36-4 F: C331H467N73O89S10 W: 7213.34