AG-13958  (Synonyms: AG-013958)

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

467.50

C₂₆H₂₂FN₇O

319460-94-1

Solid

White to off-white

O=C(C1=CC(C)=NN1C)NC2=CC(NC3=CC4=C(C=C3)C(/C=C/C5=NC=CC=C5)=NN4)=CC=C2F

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [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.  [Content Brief]