TG 100572 Hydrochloride
Catalog No. T13156L CAS
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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TG 100572 Hydrochloride, CAS 867331-64-4
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Biological Description
Chemical Properties
Storage
& Solubility Information
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, FGFR2:16 nM, VEGFR2:7 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) causes significant suppression of CNV, but with an associated weight loss suggestive of systemic toxicity[1]. TG 100572(23.4 μM) 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, TG 100572 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[2]. |
Molecular Weight |
512.43
|
Formula |
C26H27Cl2N5O2 |
CAS No. |
867331-64-4 |
Storage
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
Solubility Information
DMSO: 20 mg/mL (39.03 mM),
Need ultrasonic
( < 1 mg/ml refers to the product slightly soluble or insoluble )
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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.
Keywords
TG 100572 Hydrochloride
867331-64-4
蛋白酪氨酸激酶
血管生成
FGFR
PDGFR
Src
VEGFR
Vascular endothelial growth factor receptor
TG100572
Inhibitor
TG 100572
Platelet-derived growth factor receptor
inhibit
Fibroblast growth factor receptor
TG-100572
inhibitor