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TG 100572 Hydrochloride

Catalog No. T13156LCas No. 867331-64-4

TG 100572 Hydrochloride 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 Hydrochloride

TG 100572 Hydrochloride

Purity: 98%
Catalog No. T13156LCas No. 867331-64-4
TG 100572 Hydrochloride 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).
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1 mg$399In Stock
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Purity:98%
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Product Introduction

Bioactivity
Description
TG 100572 Hydrochloride 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
FGFR1:2 nM, PDGFRβ:13 nM, VEGFR1:2 nM, VEGFR2:7 nM, FGFR2:16 nM
In vitro
apoptosis in rapidly proliferating, but not quiescent, endothelial cell cultures induced by TG 100572[1]. TG 100572 is shown to inhibit hRMVEC cell proliferation(IC50 of 610±72 nM). TG 100572 has the therapeutic potential to inhibit VEGF function in ocular endothelial cells, a contributing factor to pathological angiogenesis in diseases such as AMD and PDR[2].
In vivo
Systemic delivery of TG 100572 in a murine model of laser-induced choroidal neovascularization (CNV) significantly suppresses CNV, but is associated with weight loss indicative of systemic toxicity[1]. TG 100572 (23.4 μM) reaches the choroid and sclera within 30 minutes (Tmax = 0.5 h), with relatively low levels in the retina. Due to its short half-life in ocular tissues, TG 100572 is administered topically at least t.i.d. to maintain appropriate eye levels. The maximum concentration achievable in formulations is 0.7% w/v[2].
Chemical Properties
Molecular Weight512.43
FormulaC26H27Cl2N5O2
Cas No.867331-64-4
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 20 mg/mL (39.03 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.9515 mL9.7574 mL19.5149 mL97.5743 mL
5 mM0.3903 mL1.9515 mL3.9030 mL19.5149 mL
10 mM0.1951 mL0.9757 mL1.9515 mL9.7574 mL
20 mM0.0976 mL0.4879 mL0.9757 mL4.8787 mL

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TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments 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 DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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