PeptideDB

BT1718

CAS: 2227366-66-5 F: C159H218ClN31O47S5 W: 3511.39

BT1718 is a bicyclic anticancer peptide targeting MT1-MMP. BT1718 uses MT1-MMP to target tumors and promote delivery of
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Bioactivity BT1718 is a bicyclic anticancer peptide targeting MT1-MMP. BT1718 uses MT1-MMP to target tumors and promote delivery of the cytotoxic payload Mertansine (HY-19792). BT1718 is a bicycle toxin conjugate with a KD value of 3 nM. MT1-MMP is overexpressed in a variety of advanced solid tumors, including triple-negative breast cancer (TNBC), non-small cell lung cancer[1][2].
Invitro BT1718 (IC50=1 nM, 72 h) 在 ATP 终点测定实验中显示出对 HT-1080 细胞细胞毒性[2]。
In Vivo BT1718 (10mg/kg, 静脉注射, 每周三次) 在植入 MT1 阳性 EBC-1 细胞的小鼠的细胞衍生异种移植模型中显示出快速的肿瘤清除作用[2]。BT1718 (10mg/kg, 静脉注射, 每周一次或每周两次) 在植入 MT1 阳性的 HT-1080 细胞的小鼠的细胞衍生异种移植模型中显示肿瘤完全清除作用[2]。 Animal Model:
Name BT1718
CAS 2227366-66-5
Formula C159H218ClN31O47S5
Molar Mass 3511.39
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]. Gowland C, et al. Development of a LC-MS/MS method for the quantification of toxic payload DM1 cleaved from BT1718 in a Phase I study. Bioanalysis. 2021 Jan;13(2):101-113. [2]. Helen Harrison, et al. BT1718, a novel bicyclic peptide-maytansinoid conjugate targeting MT1-MMP for the treatment of solid tumors: Design of bicyclic peptide and linker selection.Cancer Research 77(13 Supplement) 2017 July:5144-5144