| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 500mg | |||
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| Targets |
AG1433 targets the receptor tyrosine kinases PDGFRβ (platelet-derived growth factor receptor beta) and VEGFR-2 (vascular endothelial growth factor receptor 2, also known as Flk-1/KDR). It inhibits these kinases with IC50 values of 5.0 μM and 9.3 μM, respectively. By preventing their activation, it blocks downstream signaling pathways that promote endothelial cell proliferation and migration, thereby inhibiting angiogenesis.
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| ln Vitro |
Treatment of glioblastoma cells with tyrophostin AG1433 (0.1-100 μM; 72 hours; GB8B cells) causes moderate cytotoxicity [1].
In vitro, Tyrphostin AG1433 selectively inhibits PDGFRβ and VEGFR-2 with IC50 values of 5.0 μM and 9.3 μM, respectively. It prevents angiogenesis by inhibiting these key receptor tyrosine kinases. It has been used as a research tool to investigate the role of these kinases in various cellular processes, including cell growth, migration, and signal transduction. |
| ln Vivo |
Angiogenesis was examined using the Chorioallantoic membrane (CAM) assay to evaluate the impact of Flk-i inhibitors. Tyrphostin AG1433 (SU1433) is suited for CAM in chicken embryos that are 4-6 days old and is made from methylcellulose particles. Under the particles, tyrosine phosphatase AG1433 inhibits the growth of new fish algae [2].
In vivo, Tyrphostin AG1433 has been shown to prevent angiogenesis in models such as the chicken embryo chorioallantoic membrane (CAM) assay. By inhibiting PDGFRβ and VEGFR-2, it can reduce tumor growth and metastasis in animal models. Its anti-angiogenic properties make it a valuable tool for studying the role of angiogenesis in cancer and other diseases. |
| Enzyme Assay |
In vitro enzyme assays for Tyrphostin AG1433 involve kinase inhibition studies using recombinant PDGFRβ and VEGFR-2. The kinases are incubated with increasing concentrations of the compound, ATP, and specific peptide substrates. Phosphorylation is measured using radioactive ³³P-ATP or through luminescence-based assays. IC50 values of 5.0 μM for PDGFRβ and 9.3 μM for VEGFR-2 are determined from dose-response curves.
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| Cell Assay |
Cell viability assay [1]
Cell Types: GB8B Cell Tested Concentrations: 0.1 μM, 1 μM, 5 μM, 10 μM, 20 μM, 30 μM, 50 μM, 60 μM, 100 μM Incubation Duration: 72 hrs (hours) Experimental Results: Significant induction Cell death occurred in a concentration-dependent manner in GB8B cells. For in vitro cell-based assays, endothelial cells (e.g., HUVECs) are cultured and treated with Tyrphostin AG1433. Its anti-angiogenic activity is assessed by measuring its effects on endothelial cell proliferation, migration, and tube formation. Cell viability is assessed by MTT assays. The inhibition of PDGFR and VEGFR signaling is confirmed by Western blot for phosphorylated receptors and downstream signaling proteins. |
| Animal Protocol |
In vivo animal studies with Tyrphostin AG1433 typically use the chicken embryo chorioallantoic membrane (CAM) assay to assess its anti-angiogenic effects. It is also tested in mouse xenograft models of cancer, where it is administered orally or intraperitoneally. Tumor growth, angiogenesis, and metastasis are monitored. The compound's effects on blood vessel formation are assessed by immunohistochemistry for endothelial cell markers.
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| ADME/Pharmacokinetics |
Tyrphostin AG1433 (CAS: 168835-90-3) has a molecular weight of 266.29 g/mol and a molecular formula of C16H14N2O2. It is also known as SU1433. It is a solid and is typically stored as a powder. It is soluble in DMSO. The compound is a selective inhibitor of PDGFRβ and VEGFR-2 with anti-angiogenic properties.
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| Toxicity/Toxicokinetics |
As a tyrosine kinase inhibitor, Tyrphostin AG1433 may have off-target effects at higher concentrations. In preclinical studies, it has shown a manageable safety profile. It is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling the compound.
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| References | |
| Additional Infomation |
Tyrphostin AG 1433 is a member of the Tyrphostin family of tyrosine kinase inhibitors that selectively inhibit platelet-derived growth factor β receptor kinase and angiogenesis. (National Cancer Institute)
AG1433 is a tyrosine kinase inhibitor that selectively targets PDGFRβ and VEGFR-2 with IC50 values of 5.0 μM and 9.3 μM, respectively. It prevents angiogenesis and is used as a research tool to study these kinases. It is not an FDA-approved drug and is intended for research use only. |
| Molecular Formula |
C16H14N2O2
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|---|---|
| Molecular Weight |
266.29456
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| Exact Mass |
266.105
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| CAS # |
168835-90-3
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| PubChem CID |
2050
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| Appearance |
Light yellow to khaki solid powder
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| LogP |
2.9
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
20
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| Complexity |
338
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC2=NC=C(N=C2C=C1C)C3=CC(=C(C=C3)O)O
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| InChi Key |
SMKFYHOKXJUJOT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H14N2O2/c1-9-5-12-13(6-10(9)2)18-14(8-17-12)11-3-4-15(19)16(20)7-11/h3-8,19-20H,1-2H3
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| Chemical Name |
4-(6,7-dimethylquinoxalin-2-yl)benzene-1,2-diol
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| Synonyms |
Tyrphostin AG1433; Tyrphostin AG-1433
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~62.5 mg/mL (~234.71 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.81 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7553 mL | 18.7765 mL | 37.5530 mL | |
| 5 mM | 0.7511 mL | 3.7553 mL | 7.5106 mL | |
| 10 mM | 0.3755 mL | 1.8777 mL | 3.7553 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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