Angiopep-2-Cys

Angiopep-2-Cys is a conjugate of Angiopep-2 hydrochloride (HY-P2341) and cysteine. Angiopep-2-Cys binds to low-density lipoprotein receptors, promotes the penetration of related nanoplatforms across the blood-brain barrier, and is taken up by glioblastoma cells and cerebrovascular endothelial cells. Angiopep-2-Cys can be used in research related to glioblastoma multiforme^[1][2]. In Vitro:Angiopep-2-Cys (6 mg; 12 h stirred at 37°C) successfully conjugates to DSPE-PEG-Mal to form DSPE-PEG-Angiopep-2 for nanoparticle surface modification^[1].
Angiopep-2-Cys (5 μg/mL ICG equivalent AM-NP; 1 h) modified AM-NP exhibits enhanced, target-specific uptake by GL261 mouse glioblastoma cells via Angiopep-2 receptor interactions^[1].
Angiopep-2-Cys (10 μg/mL ICG equivalent AM-NP; 4 h) modified AM-NP enhances penetration across a bEnd.3 cell-based in vitro BBB model via receptor-mediated transcytosis^[1]. In Vivo:The Angiopep-2-Cys-modified nanoplatform (AM-NP) (5 mg/kg; i.v., tail vein injection; 3 doses (day 10, 13, 16 post-tumor inoculation)) achieves targeted brain tumor accumulation, extends median mouse survival by about 7 days when combined with 808 nm laser irradiation, induces potent tumor site hyperthermia, reduces tumor burden, and exhibits excellent in vivo biocompatibility^[1].
The Angiopep-2-Cys-modified nanoplatform (AM-NP) (5 mg/kg; i.v., tail vein injection; single dose) prolongs plasma circulation half-life to 5.278 h and enhances brain accumulation relative to non-targeted controls^[1].
Angiopep-2-Cys (5.0-50 mg/kg BPA equivalent; i.v. via tail vein; single dose)-conjugated Nano-Boron selectively accumulates in intracranial glioblastoma tumors in athymic NCr-nu/nu mice at a 16.2:1 tumor-to-healthy brain ratio, crosses the blood-brain barrier, and localizes intracellularly within tumor cells^[2].