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TG 100801

Catalog No. T13157 CAS 867331-82-6

Synonyms: TG100801, TG 100572

TG 100801 is a dual inhibitor of VEGFr2 and Src family (Src and YES) kinases and is a candidate compound for the treatment of age-related macular degeneration (AMD).

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TG 100801, CAS 867331-82-6

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2 mg	In stock	$ 123.00

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Purity: 100%

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Description	TG 100801 is a dual inhibitor of VEGFr2 and Src family (Src and YES) kinases and is a candidate compound for the treatment of age-related macular degeneration (AMD).
Targets&IC50	PDGFRβ:13 nM, FGFR1:2 nM, FGFR2:16 nM, VEGFR1:2 nM, VEGFR2:7 nM
In vitro	TG100801 is a locally administered prodrug that readily converts to active TG100572. TG100572 inhibits endothelial cell proliferation in vitro (ED50 = 610 ± 71 nM) and blocks the phosphorylation of extracellular signal-regulated kinase (ERK) induced by VEGF [2].
In vivo	TG 100801 is formed by derivatizing the phenol moiety in TG100572 to produce an ester, striking an optimal balance between stability (physical and chemical) and hydrolysis rate among the prodrugs examined. TG100801 does not exhibit meaningful kinase activity but exposure to esterases (abundant in mammalian tissues) rapidly releases active TG 100572. Mice receiving daily intraperitoneal injections of TG 100572 (5 mg/kg) display smaller CNV lesions compared to vehicle-injected mice[2].

Synonyms	TG100801, TG 100572
Molecular Weight	580.08
Formula	C33H30ClN5O3
CAS No.	867331-82-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 3 mg/mL (5.17 mM), Sonication is recommended.

H2O: < 0.1 mg/mL (insoluble)

References and Literature

1. 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. 2. Doukas, John, et al. Topical administration of a multi-targeted kinase inhibitor suppresses choroidal neovascularization and retinal edema. Journal of Cellular Physiology (2008), 216(1), 29-37.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Drug Repurposing Compound Library Inhibitor Library

Related Products

Related compounds with same targets

Regorafenib VEGFR2/HDAC1-IN-1 hCA/VEGFR-2-IN-4 SCR-1481B1 AKB-6899 Linifanib VEGFR-2-IN-33 Jaceidin

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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 100801 867331-82-6 Angiogenesis Tyrosine Kinase/Adaptors VEGFR Src TG100801 TG 100572 TG-100801 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.