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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $84 | In Stock | |
5 mg | $198 | In Stock | |
10 mg | $292 | In Stock | |
25 mg | $492 | In Stock | |
50 mg | $717 | In Stock | |
100 mg | $987 | In Stock | |
500 mg | $1,980 | In Stock |
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). |
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]. |
Alias | 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 | Shipping with blue ice. | |||||||||||||||
Solubility Information | DMSO: 3 mg/mL (5.17 mM), Sonication is recommended. H2O: < 0.1 mg/mL (insoluble) | |||||||||||||||
Solution Preparation Table | ||||||||||||||||
DMSO
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