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TG 100801
Catalog No. T13157Cas No. 867331-82-6
Alias 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).
TG 100801
Catalog No. T13157Alias TG100801, TG 100572Cas No. 867331-82-6
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).
| 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 |
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Purity:100%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| 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 | FGFR1:2 nM, PDGFRβ:13 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]. |
| Alias | TG100801, TG 100572 |
| Molecular Weight | 580.08 |
| Formula | C33H30ClN5O3 |
| Cas No. | 867331-82-6 |
Storage & Solubility Information
| 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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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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