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TG 100572 Hydrochloride

Catalog No. T13156L   CAS 867331-64-4
Synonyms: Vascular endothelial growth factor receptor, FGFR, TG100572, PDGFR, Inhibitor, TG 100572 Hydrochloride, TG 100572, VEGFR, Platelet-derived growth factor receptor, inhibit, Fibroblast growth factor receptor, TG-100572, Src

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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Purity: 98%
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].
Synonyms Vascular endothelial growth factor receptor, FGFR, TG100572, PDGFR, Inhibitor, TG 100572 Hydrochloride, TG 100572, VEGFR, Platelet-derived growth factor receptor, inhibit, Fibroblast growth factor receptor, TG-100572, Src
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 )

Citations

References and Literature
1. Doukas J, 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. 2. Palanki MS, et al. Development of prodrug 4-chloro-3-(5-methyl-3-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}-1,2,4-benzotriazin-7-yl)phenyl benzoate (TG100801): a topically administered therapeutic candidate in clinical trials for the treatment of age-related macular degeneration. J Med Chem. 2008 Mar 27;51(6):1546-59.

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