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| 25mg |
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| 50mg |
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Purity: ≥98%
Tyrphostin AG 1296 (AG-1296) is a novel, potent, selective and ATP-competitive inhibitor of PDGFR with potential antitumor activity. It exhibits no activity against EGFR and inhibits PDGFR with an IC50 of 0.3-0.5 μM. Tyrphostin AG 1296 functions by binding to PDGFR and causing the ATP-binding site to undergo a conformational change. It effectively prevents the ligand-induced autophosphorylation of the PDGF receptor in Swiss 3T3 cell membranes in an in vitro experiment. Up to 100μM of tyrphostin AG 1296 does not interfere with the EGF receptor. Tyrphostin AG 1296 likewise prevents PDGF-induced mitogenesis, but not insulin or EGF-induced mitogenesis. With an IC50 mean of 1.5μM, it reversibly inhibits PDGF-induced DNA synthesis.
| Targets |
PDGFR (IC50 = 0.3 μM-0.5 μM); c-Kit (IC50 = 1.8 μM); FGFR (IC50 = 12.3 μM)
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
Confluent cultures of Swiss 3T3 cells are used to prepare membranes, as explained. A 45μl volume containing 10μg of membrane protein per assay, 50 mM Hepes (pH 7.5), 2μg/mL PDGF, or both, and 3 mM MnCl2 is added. The mixture is then incubated for 20 minutes on ice. This allows for the measurement of receptor autophosphorylation. Tyrphostins are added 15 minutes before the growth factors are added, in a volume of 0.5 μl (in DMSO; final concentration, 0.5%), to test their effects. The addition of [γ-32P]ATP starts the phosphorylation process, which is stopped after two minutes by adding 10μL of a solution that contains 0.6 SDS, 30%β-mercatoethanol, 40% glycerol, and 0.5 mg/mL bromophenol blue. The gels undergo autoradiographic analysis after being dried, stained, and processed.
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| Cell Assay |
In 24-well plates, 5000 cells per well are seeded with DMEM/10% FCS. The medium is switched to DMEM/2% FcS the following day, either with or without growth factors, and tyrphostins are added as needed. The cells are counted in a hemocytometer three days later.
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| Animal Protocol |
Nud/nud mice are injected with A375R cells
40, 80 mg/kg I.p. daily for two weeks |
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| References | ||
| Additional Infomation |
6,7-dimethoxy-2-phenylquinoxaline is a quinoxaline derivative.
Tyrphostin AG 1296 is a member of the tyrphostin family of tyrosine kinase inhibitors that selectively inhibits platelet-derived growth factor receptor protein. (NCI) |
| Molecular Formula |
C16H14N2O2
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| Molecular Weight |
266.29
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| Exact Mass |
266.105
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| Elemental Analysis |
C, 72.16; H, 5.30; N, 10.52; O, 12.02
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| CAS # |
146535-11-7
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| Related CAS # |
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| PubChem CID |
2049
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
420.2±40.0 °C at 760 mmHg
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| Flash Point |
151.8±17.6 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.618
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| LogP |
3.76
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
20
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| Complexity |
307
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(C([H])([H])[H])C1=C(C([H])=C2C(=C1[H])N=C(C([H])=N2)C1C([H])=C([H])C([H])=C([H])C=1[H])OC([H])([H])[H]
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| InChi Key |
QNOXYUNHIGOWNY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H14N2O2/c1-19-15-8-12-13(9-16(15)20-2)18-14(10-17-12)11-6-4-3-5-7-11/h3-10H,1-2H3
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| Chemical Name |
6,7-dimethoxy-2-phenylquinoxaline
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (9.39 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.39 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (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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