TG 100801

TG 100801 is a proagent that generates TG 100572 by de-esterification in development to treat age-related macular degeneration. TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.

Product Specifications

CAS Number

[867331-82-6]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

FGFR; PDGFR; Src; VEGFR

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/TG-100801.html

Purity

98.61

Solubility

DMSO : 5.56 mg/mL (ultrasonic)

Smiles

O=C(C1=CC=CC=C1)OC2=CC=C(Cl)C(C3=CC(C)=C(N=C(NC(C=C4)=CC=C4OCCN5CCCC5)N=N6)C6=C3)=C2

Molecular Formula

C33H30ClN5O3

Molecular Weight

580.08

Precautions

H302, H315, H319, H335

References & Citations

[1]Palanki MS, et al. Development of prodrug 4-chloro-3- (5-methyl-3-{[4- (2-pyrrolidin-1-ylethoxy) phenyl]amino}-1,2,4-benzotriazin-7-yl) phenyl benzoate (TG100801) : a topically administered therapeutic candidate in clinical trials for the treatment of age-related macular degeneration. J Med Chem. 2008 Mar 27;51 (6) :1546-59.|[2]Doukas, John, et al. Topical administration of a multi-targeted kinase inhibitor suppresses choroidal neovascularization and retinal edema. Journal of Cellular Physiology (2008), 216 (1), 29-37.