For research use only. Not for therapeutic Use.
AG-13958 (AG-013958), a potent VEGFR tyrosine kinase inhibitor, is used for treatment of choroidal neovascularization associated with age-related macular degeneration (AMD)[1].
AG-13958 (AG-013958) is ATP-competitive by tight-binding kinetic analysis when minigastrin (0.5 mM) is used as a substrate[2].
ST administration (Steroid injection) of AG-13958 suspension produces a depot of drug on the posterior surface of the sclera that provided sustained exposure to the choroid with little impact on peripheral tissues and no measurable systemic exposure[1].
| Catalog Number | I001401 |
| CAS Number | 319460-94-1 |
| Synonyms | N-[2-fluoro-5-[[3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl]amino]phenyl]-2,5-dimethylpyrazole-3-carboxamide |
| Molecular Formula | C26H22FN7O |
| Purity | ≥95% |
| InChI | InChI=1S/C26H22FN7O/c1-16-13-25(34(2)33-16)26(35)30-24-15-19(7-10-21(24)27)29-18-6-9-20-22(31-32-23(20)14-18)11-8-17-5-3-4-12-28-17/h3-15,29H,1-2H3,(H,30,35)(H,31,32)/b11-8+ |
| InChIKey | JXSVVZKPEDIRTN-DHZHZOJOSA-N |
| SMILES | CC1=NN(C(=C1)C(=O)NC2=C(C=CC(=C2)NC3=CC4=C(C=C3)C(=NN4)C=CC5=CC=CC=N5)F)C |
| Reference | [1]. M.B. Kosa, et al. Ocular and Systemic Pharmacokinetics of AG-013958 With Sub-Tenon Administration To Cynomologus Monkeys. Investigative Ophthalmology & Visual Science May 2005, Vol.46, 5379. [2]. Solowiej J, et al. Substrate-specific conformational regulation of the receptor tyrosine kinase VEGFR2 catalytic domain. ACS Chem Biol. 2013 May 17;8(5):978-86. |
