TG 100572 Inhibitor CAS No. 867334-05-2

Cat. No.	Name	Size	Price
KI2050	TG 100572	5 mg	$800.8
	TG 100572	10 mg	$1573
	TG 100572	200 mg	$6292

Chemical Characteristic

Product Name	TG 100572
Synonyms	N/A
CAS No.	867334-05-2
Molecular Weight	475.97
Formula	C₂₆H₂₆ClN₅O₂
Chemical Name	4-chloro-3-[5-methyl-3-[4-(2-pyrrolidin-1-ylethoxy)anilino]-1,2,4-benzotriazin-7-yl]phenol
Smiles	c1(cc(c(cc1)Cl)c1cc(c2nc(nnc2c1)Nc1ccc(cc1)OCCN1CCCC1)C)O
Chemical Structure

Biological activities

TG 100572 is VEGFR2 and Src kinase inhibitor. In vitro, TG 100572 controls the lesion severity independent of herpes simplex virus (HSV) replication. TG 100572 inhibits CD4⁺ T cell proliferation in vitro. In addition, TG 100572 administration down-regulates CD49d on CD4⁺T cells in lymphoid organs, resulting in fewer cells to migrate to the ocular site. In C57BL/6 animals infected with HSV in vivo, TG 100572 administration markedly diminishes levels of HSV-induced angiogenesis.^[1] In a murine model of laser-induced choroidal neovascularization (CNV), TG 100572 treatment significantly suppresses CNV, but with an associated weight loss suggestive of systemic toxicity.^[2]

Protocols

TG 100572 is prepared for in vitro assays as DMSO stocks, for i.p. delivery as Solutol:polyethylene glycol 400: ethanol: water solutions (10:10:10:70, pH 5), and for topical delivery as sterile-filtered aqueous-based solutions containing 1% hydroxypropyl methyl cellulose, 0.2% tyloxapol, 3.4% dextrose, 0.006% benzalkonium chloride, and 0.025% ethylenediaminetetraacetic acid (280 mOsm, pH 5.4).^[2]

References

[1] Sharma S et al. An anti-inflammatory role of VEGFR2/Src kinase inhibitor in herpes simplex virus 1-induced immunopathology. J Virol. 2011, 85(12): 5995-6007. [2] Doukas J et al. Topical administration of a multi-targeted kinase inhibitor suppresses choroidal neovascularization and retinal edema. J Cell Physiol. 2008, 216(1): 29-37.

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