| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
Platelet-derived growth factor receptor (PDGFR) tyrosine kinase.
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| ln Vitro |
AG 1295 suppresses PDGFR autophosphorylation, membrane autophosphorylation and the IC50 observed in Swiss 3T3 cells are 0.3-0.5 μM and 0.5-1 μM correspondingly [1]. AG1295 (10 μM, 100 μM) greatly reduces cell viability assay in vitro [2]
In vitro, AG 1295 inhibits PDGFR tyrosine kinase activity, blocking receptor autophosphorylation and downstream signaling. The compound inhibits PDGF-dependent DNA synthesis with an IC₅0 of 2.5 microM in Swiss 3T3 cells. AG 1295 is a potent blocker of smooth muscle cell proliferation. It shows no effect on EGF receptor autophosphorylation, confirming its selectivity for PDGFR. The compound has been investigated for potential therapeutic applications in atherosclerosis, restenosis, pulmonary fibrosis, and glioma. |
| ln Vivo |
In aortic allograft vascular damage, AG-1295 inhibits tyrosine phosphorylation caused by PDGFR-β, hence reducing neointima. AG1295 (12 mg/kg; intraperitoneal; daily; 14 or 21 days) was found to dramatically reduce interstitial fibrosis, as seen by larger regions stained with Sirius red, a decrease in macrophage counts, ED-A+ fibronectin deposition, and α-Smooth muscle actin-promoting protein cell counts [4].
In vivo, AG 1295 has been studied in various disease models including atherosclerosis, restenosis, pulmonary fibrosis, and glioma. Its PDGFR inhibitory activity makes it a valuable tool for studying the role of PDGFR signaling in these pathological conditions. Detailed in vivo efficacy data depend on the specific model used. |
| Enzyme Assay |
Kinase inhibition assays are performed using purified PDGFR kinase or immunoprecipitated PDGFR from cell lysates. The kinase reaction mixture contains 20 mM HEPES (pH 7.4), 10 mM MgCl2, 10 mM MnCl2, 1 mM DTT, 0.1 mM ATP (with [gamma-32P]ATP), and a peptide substrate (e.g., poly(Glu,Tyr) 4:1). AG 1295 is added at concentrations ranging from 0.01-10 microM. The reaction is initiated by adding substrate, incubated at 30degC for 15-30 minutes, and terminated by spotting onto phosphocellulose paper or by SDS-PAGE. Radioactivity incorporated into substrate is quantified. IC₅0 values are calculated from dose-response curves. Autophosphorylation assays are performed using immunoprecipitated PDGFR; phosphorylation is detected by Western blot using anti-phosphotyrosine antibodies.
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: rabbit conjunctival fibroblasts Tested Concentrations: 1 μM, 10 μM, 100 μM Incubation Duration: 3 days Experimental Results: Inhibition of PDGF-AA or PDGF -BB-stimulated growth of rabbit conjunctival fibroblasts [2]. PDGF-AA or PDGF-BB stimulates the growth of rabbit conjunctival fibroblasts. Cells expressing PDGFR (e.g., Swiss 3T3 fibroblasts, vascular smooth muscle cells, or PDGFR-transfected cells) are serum-starved for 16-24 hours and treated with AG 1295 at concentrations ranging from 0.1-10 microM for 1-2 hours. Cells are then stimulated with PDGF (10-50 ng/mL) for 5-15 minutes. PDGFR autophosphorylation is assessed by immunoprecipitation followed by Western blot with anti-phosphotyrosine antibodies. Downstream signaling (e.g., ERK, AKT phosphorylation) is assessed by Western blot. PDGF-dependent DNA synthesis is measured by [3H]-thymidine incorporation: cells are treated with AG 1295 and PDGF, incubated with [3H]-thymidine for 4-6 hours, and incorporated radioactivity is measured by scintillation counting. Cell proliferation is assessed by cell counting or MTT assays. |
| Animal Protocol |
Animal/Disease Models: SD (SD (Sprague-Dawley)) rats (240-270 g) [4]
Doses: 12 mg/kg Route of Administration: intraperitoneal (ip) injection; daily; continued for 14 or 21 days Experimental Results: Rat renal interstitial fibers after unilateral obstruction Weakened. In vivo efficacy is evaluated in animal models of diseases involving PDGFR signaling. For restenosis models, rats or mice undergo balloon injury of the carotid artery, and AG 1295 is administered systemically (oral or intraperitoneal) or locally (via drug-eluting stent or perivascular delivery). Neointima formation is assessed by histomorphometry. For glioma models, tumor-bearing mice are treated with AG 1295 and tumor growth is monitored. Doses typically range from 10-50 mg/kg administered daily or every other day. Pharmacokinetic studies are performed to determine plasma drug concentrations. |
| ADME/Pharmacokinetics |
AG 1295 has molecular formula C1₆H13N3O2 and molecular weight 279.29. It is a small-molecule tyrosine kinase inhibitor with moderate lipophilicity. The compound is soluble in DMSO and other organic solvents. Pharmacokinetic parameters (oral bioavailability, half-life, clearance) are not extensively reported in publicly available literature. The compound is typically administered parenterally for in vivo studies.
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| Toxicity/Toxicokinetics |
No specific toxicity data are reported for AG 1295. As a tyrosine kinase inhibitor, it may have off-target effects at high concentrations. The compound is for research use only and not for human therapeutic use. Standard safety precautions for handling kinase inhibitors should be observed.
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| References |
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| Additional Infomation |
6,7-Dimethyl-2-phenylquinoxaline is a quinoxaline derivative with anti-aging effects. Tyrosine kinase inhibitor AG 1295 belongs to the tyrosine kinase inhibitor family; it inhibits platelet-derived growth factor receptor signal transduction and selectively attenuates smooth muscle cell growth. (NCI)
AG 1295 (Tyrphostin AG 1295) is a selective PDGFR tyrosine kinase inhibitor used as a research tool to study PDGFR signaling. It inhibits PDGFR autophosphorylation with IC₅0 of 0.3-0.5 microM and PDGF-dependent DNA synthesis with IC₅0 of 2.5 microM. The compound has no effect on EGF receptor autophosphorylation, demonstrating selectivity. AG 1295 has been investigated for potential therapeutic applications in atherosclerosis, restenosis, pulmonary fibrosis, and glioma. It is not an approved therapeutic agent; it is a research compound for studying PDGFR biology. |
| Molecular Formula |
C16H14N2
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|---|---|
| Molecular Weight |
234.29600
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| Exact Mass |
234.115
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| Elemental Analysis |
C, 82.02; H, 6.02; N, 11.96
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| CAS # |
71897-07-9
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| PubChem CID |
2048
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
398.3±37.0 °C at 760 mmHg
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| Flash Point |
172.4±17.8 °C
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| Vapour Pressure |
0.0±0.9 mmHg at 25°C
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| Index of Refraction |
1.636
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| LogP |
3.92
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
18
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| Complexity |
272
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1C2C(=CC(C)=C(C)C=2)N=CC=1C1=CC=CC=C1
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| InChi Key |
FQNCLVJEQCJWSU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H14N2/c1-11-8-14-15(9-12(11)2)18-16(10-17-14)13-6-4-3-5-7-13/h3-10H,1-2H3
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| Chemical Name |
6,7-dimethyl-2-phenylquinoxaline
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| Synonyms |
AG1295; AG-1295; AG 1295; NSC 380341; Tyrphostin AG 1295.
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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 (~266.75 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.88 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (8.88 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (8.88 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.2680 mL | 21.3402 mL | 42.6803 mL | |
| 5 mM | 0.8536 mL | 4.2680 mL | 8.5361 mL | |
| 10 mM | 0.4268 mL | 2.1340 mL | 4.2680 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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