N-[2-Fluoro-5-[[3-[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]amino]phenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide
N-[2-Fluoro-5-[[3-[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]amino]phenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide Basic information
- Product Name:
- N-[2-Fluoro-5-[[3-[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]amino]phenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide
- Synonyms:
-
- N-[2-Fluoro-5-[[3-[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]amino]phenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide
- AG 13958
- AG-013958
- N-[2-Fluoro-5-({3-[(E)-2-(2-pyridinyl)vinyl]-1H-indazol-6-yl}amin o)phenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide
- (E)-N-(2-Fluoro-5-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)amino)phenyl)-1,3-dimethyl-1H-py
- (E)-N-(2-Fluoro-5-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)amino)phenyl)-1,3-dimethyl-1H-pyrazole-5-carboxamide
- AG13958 ≥95%
- AG 13958;AG-13958
- CAS:
- 319460-94-1
- MF:
- C26H22FN7O
- MW:
- 467.5
- Mol File:
- 319460-94-1.mol
N-[2-Fluoro-5-[[3-[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]amino]phenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide Chemical Properties
- Boiling point:
- 647.8±55.0 °C(Predicted)
- Density
- 1.35±0.1 g/cm3(Predicted)
- storage temp.
- 4°C, protect from light
- solubility
- DMSO: 5 mg/mL (10.70 mM; ultrasonic and warming and heat to 60°C)
- form
- Solid
- pka
- 12.13±0.70(Predicted)
- color
- White to off-white
N-[2-Fluoro-5-[[3-[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]amino]phenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide Usage And Synthesis
Uses
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].
in vivo
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].
IC 50
VEGFR
References
[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. DOI:10.1021/cb400040z
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