TG 100572
Based on 3 publication(s) in Google Scholar
TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
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- CAS No.: 867334-05-2
- Formule: C26H26ClN5O2
- Masse moléculaire:475.97
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) TG 100572
MoreVoir tous les produits spécifiques à Isoform VEGFR
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Activité biologique
|
VEGFR1 2 nM (IC50) |
VEGFR2 7 nM (IC50) |
FGFR1 2 nM (IC50) |
FGFR2 16 nM (IC50) |
PDGFRβ 13 nM (IC50) |
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[1]. 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[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 867334-05-2
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Masse moléculaire 475.97
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Formule C26H26ClN5O2
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SMILES
ClC1=CC=C(O)C=C1C2=CC(C)=C(N=C(NC(C=C3)=CC=C3OCCN4CCCC4)N=N5)C5=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (3)
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Journal Impact Factor
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Most Recent
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Science
2017 Dec 1;358(6367):eaan4368. PMID: 29191878 -
ACS Appl Mater Interfaces
Resveratrol-Loaded PLGA Enhanced Vitrified Oocyte Viability through Rab11fip4/Arf5-Mediated Internalization Route. [Abstract]2025 Aug 6;17(31):44160-44177. PMID: 40720586 -
Am J Pathol
Antitumor Activity of a Novel Fibroblast Growth Factor Receptor Inhibitor for Intrahepatic Cholangiocarcinoma. [Abstract]2019 Oct;189(10):2090-2101. PMID: 31351075
Solvant et solubilité
DMSO : ≥ 150 mg/mL (315.15 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocole
For proliferation assays, human retinal microvascular EC plated in 96-well cluster plates are cultured for 48 hr in the presence of either TG 100572 (2 nM-5 µM) or DMSO; medium contained 10% FBS, 50 µg/mL heparin, and 50 ng/mL rhVEGF. Cell numbers are then assessed using an XTT-based assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: C57BL/6 mice (15-20 g) are dosed i.p. twice daily for 4 days with 5 mg/ kg TG 100572, followed by a single dose on Day 5, 5 hr after which plasma samples are taken, animals euthanized, and eyes explanted. Alternatively, mice are dosed topically with either TG 100572 or related prodrugs (e.g., TG 100801) by delivering a single 10 µL drop to both eyes for a total of two days, and both plasma and eyes harvested prior to or 0.5, 1, 3, 5, or 7 hr after the Day 2 dosing[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
Références
[1]. Doukas J, et al. Topical administration of a multi-targeted kinase inhibitor suppresses choroidal neovascularization and retinal edema. J Cell Physiol. 2008 Jul;216(1):29-37. [Content Brief]
[2]. 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-rela [Content Brief]
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1010 mL | 10.5049 mL | 21.0097 mL | 52.5243 mL |
| 5 mM | 0.4202 mL | 2.1010 mL | 4.2019 mL | 10.5049 mL | |
| 10 mM | 0.2101 mL | 1.0505 mL | 2.1010 mL | 5.2524 mL | |
| 15 mM | 0.1401 mL | 0.7003 mL | 1.4006 mL | 3.5016 mL | |
| 20 mM | 0.1050 mL | 0.5252 mL | 1.0505 mL | 2.6262 mL | |
| 25 mM | 0.0840 mL | 0.4202 mL | 0.8404 mL | 2.1010 mL | |
| 30 mM | 0.0700 mL | 0.3502 mL | 0.7003 mL | 1.7508 mL | |
| 40 mM | 0.0525 mL | 0.2626 mL | 0.5252 mL | 1.3131 mL | |
| 50 mM | 0.0420 mL | 0.2101 mL | 0.4202 mL | 1.0505 mL | |
| 60 mM | 0.0350 mL | 0.1751 mL | 0.3502 mL | 0.8754 mL | |
| 80 mM | 0.0263 mL | 0.1313 mL | 0.2626 mL | 0.6566 mL | |
| 100 mM | 0.0210 mL | 0.1050 mL | 0.2101 mL | 0.5252 mL |
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