| Hazard Information | Back Directory | [Uses]
EG01377 is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1), with a Kd of 1.32 μM, and IC50s of both 609 nM for NRP1-a1 and NRP1-b1. EG01377 has antiangiogenic, antimigratory, and antitumor effects[1]. | [in vivo]
EG01377 (2 mg/kg; i.v.) exhibits an encouraging half-life of 4.29 h, sufficient to sustain once per day dosing in mice[1]. | Animal Model: | 6–8 week-old BABL/c female mice[1] | | Dosage: | 2 mg/kg (Pharmacokinetic Analysis) | | Administration: | I.v. administration | | Result: | The half time (T1/2) of 4.29 h. |
| [References]
[1] Powell J, et al. Small Molecule Neuropilin-1 Antagonists Combine Antiangiogenic and Antitumor Activity with Immune Modulation through Reduction of Transforming Growth Factor Beta (TGFβ) Production in Regulatory T-Cells. J Med Chem. 2018 May 10;61(9):4135- DOI:10.1021/acs.jmedchem.8b00210 |
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