TG100801
TG100801 Basic information
- Product Name:
- TG100801
- Synonyms:
-
- TG100801
- Phenol, 4-chloro-3-[5-Methyl-3-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]aMino]-1,2,4-benzotriazin-7-yl]-, 1-benzoate
- 4-Chloro-3-[5-methyl-3-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-1,2,4-benzotriazin-7-yl]phenol 1-benzoate
- 4-Chloro-3-(5-methyl-3-((4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)-amino)benzo[e][1,2,4]triazin-7-yl)p
- 4-Chloro-3-(5-methyl-3-(4-(2-(pyrrolidin-1-yl)ethoxy)phenylamino)benzo[e][1,2,4]triazin-7-yl)phenyl benzoate
- 4-Chloro-3-(5-methyl-3-((4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)-amino)benzo[e][1,2,4]triazin-7-y
- TG100801;TG-100801
- CAS:
- 867331-82-6
- MF:
- C33H30ClN5O3
- MW:
- 580.08
- Mol File:
- 867331-82-6.mol
TG100801 Chemical Properties
- Boiling point:
- 747.9±70.0 °C(Predicted)
- Density
- 1.310
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- form
- Powder
- pka
- 9.59±0.20(Predicted)
- color
- Brown to reddish brown
TG100801 Usage And Synthesis
Uses
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.
Biological Activity
tg100801 is a multi-kinases inhibitor. it is a pro-drug version of tg100572. [1]tg100572 inhibits several growth factor receptors in addition to src family kinases. tg100801 significantly inhibited laser-induced cnv in mice, and suppressed fluorescein leakage from the vasculature and retinal thickening measured by optical coherence tomography in a rat model or retinal vein occlusion. tg100801 may play as a new topically applied treatment approach for ocular neovascularization and retinal edema. the highest concentration of tg100801 was found at the front of the rat eye (conjunctiva and cornea). [1]
in vivo
TG 100801 exhibits excellent ocular pharmacokinetics and poor systemic circulation and shows good efficacy in the laser induced choroidal neovascularization model. A concentration of 23.4 μM (Cmax) of TG 100572 is reached in 30 min (Tmax)=0.5 h) in the choroid and the sclera. However, the levels of TG 100572 in the retina are relatively low. The half-life of TG 100572 in ocular tissues is very short; hence, the compound is administered topically minimum t.i.d. to maintain appropriate drug levels in the eye. The maximum concentration one can achieve in formulations using TG 100572 is 0.7% w/v[1]. TG 100801 nor TG100572 are detectable in plasma following topical delivery of TG 100801, and adverse safety signals (such as weight loss) are not observed even with prolonged dosing schedules. Topical TG 100801 significantly suppresses laser-induced choroidal neovascularlization in mice, and reduces fluorescein leakage from the vasculature and retinal thickening measured by optical coherence tomography in a rat model or retinal vein occlusion.Systemic delivery of TG 100572 in a murine model of laser-induced choroidal neovascularization (CNV) causes significant suppression of CNV, but with an associated weight loss suggestive of systemic toxicity[2].
target
VEGFR1
IC 50
VEGFR1: 2 nM (IC50); VEGFR2: 7 nM (IC50); FGFR1: 2 nM (IC50); FGFR2: 16 nM (IC50); PDGFRβ: 13 nM (IC50)
References
1. doukas j, mahesh s, umeda n et al. topical administration of a multi-targeted kinase inhibitor suppresses choroidal neovascularization and retinal edema. j cell physiol. 2008 jul;216(1):29-37.
TG100801Supplier
- Tel
- 025-58196018 800028039
- sales@fartop.net
- Tel
- 021-58950125
- info@chemexpress.com
- Tel
- 025-58849295 18951903616;
- info@adooq.cn
- Tel
- eric_feng1954@126.com
- Tel
- 020-61288194 61288195
- 505721671@qq.com