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TG 100801

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Purity:100%

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COA HNMR HPLC LCMS

TG 100801

Catalog No. T13157Cas No. 867331-82-6

TG 100801 is a dual inhibitor of VEGFr2 and Src family (Src and YES) kinases and is a candidate compound for the treatment of age-related macular degeneration (AMD).

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Pack Size	Price	Availability
1 mg	$84	In Stock
5 mg	$198	In Stock
10 mg	$292	In Stock
25 mg	$492	In Stock
50 mg	$717	In Stock
100 mg	$987	In Stock
500 mg	$1,980	In Stock

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Product Introduction

Bioactivity

Description	TG 100801 is a dual inhibitor of VEGFr2 and Src family (Src and YES) kinases and is a candidate compound for the treatment of age-related macular degeneration (AMD).
In vitro	TG100801 is a locally administered prodrug that readily converts to active TG100572. TG100572 inhibits endothelial cell proliferation in vitro (ED50 = 610 ± 71 nM) and blocks the phosphorylation of extracellular signal-regulated kinase (ERK) induced by VEGF [2].
In vivo	TG 100801 is formed by derivatizing the phenol moiety in TG100572 to produce an ester, striking an optimal balance between stability (physical and chemical) and hydrolysis rate among the prodrugs examined. TG100801 does not exhibit meaningful kinase activity but exposure to esterases (abundant in mammalian tissues) rapidly releases active TG 100572. Mice receiving daily intraperitoneal injections of TG 100572 (5 mg/kg) display smaller CNV lesions compared to vehicle-injected mice[2].
Alias	TG100801, TG 100572

Chemical Properties

Molecular Weight	580.08
Formula	C33H30ClN5O3
Cas No.	867331-82-6

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 3 mg/mL (5.17 mM)

H2O: < 0.1 mg/mL (insoluble)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
10 mM	0.1724 mL	0.8620 mL	1.7239 mL	8.6195 mL
20 mM	0.0862 mL	0.4310 mL	0.8620 mL	4.3098 mL
50 mM	0.0345 mL	0.1724 mL	0.3448 mL	1.7239 mL
100 mM	0.0172 mL	0.0862 mL	0.1724 mL	0.8620 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

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A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

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