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TG 100572

CAS No. : 867334-05-2

MCE 站：TG 100572

产品活性：TG 100572是多靶点激酶抑制剂，抑制受体酪氨酸激酶 (receptor tyrosine kinases) 和Src激酶 (Src kinases); 对VEGFR1，VEGFR2，FGFR1，FGFR2，PDGFRβ，Fgr，Fyn，Hck，Lck，Lyn，Src，Yes 的 IC₅₀ 值分别为2，7，2，16，13，5，0.5，6，0.1，0.4，1，0.2 nM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Src  |  VEGFR  |  PDGFR  |  FGFR

In Vitro: TG 100572 shows sub-nanomolar activity against the Src family as well as RTK such as VEGFR1 and R2, FGFR1 and R2, and PDGFRβ. TG 100572 inhibits vascular endothelial cell proliferation (ED₅₀=610±71 nM) and blocks VEGF-induced phosphorylation of extracellular signal-regulated kinase. TG 100572 induces apoptosis in rapidly proliferating, but not quiescent, endothelial cell cultures. TG 100572 is shown to inhibit hRMVEC cell proliferation, with an IC₅₀ of 610±72 nM. This suggests that 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.

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. A concentration of 23.4 ?M (C_max) of TG 100572 is reached in 30 min (T_max)=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, the compound 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.

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