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TG 100572

Name: TG 100572
Brand: TargetMol
SKU: T13156
Rating: 4.5 (1 reviews)

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Catalog No. T13156Cas No. 867334-05-2

TG 100572 is a inhibitor of multi-targeted kinase which inhibits receptor tyrosine kinases and Src kinases(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).

TG 100572

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Catalog No. T13156Cas No. 867334-05-2

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$1,520	6-8 weeks	6-8 weeks
50 mg	$1,980	6-8 weeks	6-8 weeks
100 mg	$2,500	6-8 weeks	6-8 weeks

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Product Introduction

Bioactivity

Description	TG 100572 is a inhibitor of multi-targeted kinase which inhibits receptor tyrosine kinases and Src kinases(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).
Targets&IC50	PDGFRβ:13 nM, FGFR1:2 nM, FGFR2:16 nM, VEGFR1:2 nM, VEGFR2:7 nM
In vitro	TG 100572 induces apoptosis in rapidly proliferating, but not quiescent, endothelial cell cultures[1]. TG 100572 is shown to inhibit hRMVEC cell proliferation with IC50 of 610±72 nM. in ocular endothelial cells,TG 100572 has the therapeutic potential to inhibit VEGF function, a contributing factor to pathological angiogenesis in diseases such as AMD and PDR[2].
In vivo	Administering TG 100572 systemically in a mouse model of laser-induced choroidal neovascularization (CNV) significantly reduces CNV but may lead to weight loss, indicating possible systemic toxicity[1]. TG 100572 reaches its peak concentration of 23.4 μM within 30 minutes (Tmax=0.5h) in the choroid and sclera, but its presence in the retina remains notably low. Due to its short half-life in ocular tissues, topical administration of TG 100572 is necessary at least three times daily (t.i.d.) to sustain effective drug levels in the eye. The maximum achievable concentration of TG 100572 in formulations is limited to 0.7% w/v[2].

Chemical Properties

Molecular Weight	475.97
Formula	C₂₆H₂₆ClN₅O₂
Cas No.	867334-05-2
Smiles	ClC1=C(C2=CC3=C(C(C)=C2)N=C(NC4=CC=C(OCCN5CCCC5)C=C4)N=N3)C=C(O)C=C1
Relative Density.	1.331 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 150 mg/mL (315.15 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1010 mL	10.5049 mL	21.0097 mL	105.0486 mL
5 mM	0.4202 mL	2.1010 mL	4.2019 mL	21.0097 mL
10 mM	0.2101 mL	1.0505 mL	2.1010 mL	10.5049 mL
20 mM	0.1050 mL	0.5252 mL	1.0505 mL	5.2524 mL
50 mM	0.0420 mL	0.2101 mL	0.4202 mL	2.1010 mL
100 mM	0.0210 mL	0.1050 mL	0.2101 mL	1.0505 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 stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc