| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
Purity: ≥98%
AG-1557 is a novel and potent inhibitor of epidermal growth factor receptor tyrosine (EGFR) kinase. The receptor family of tyrosine kinases includes the EGFR. Receptor tyrosine kinases play a role in the development of blood vessels, invasion, and proliferation of cancer cells. Overexpression of EGFR has been detected in a number of solid tumors in humans. As a result, EGFR has drawn a lot of interest as an anticancer drug target.
| Targets |
EGFR (pIC = 8.194)
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| ADME/Pharmacokinetics |
In the described high performance liquid chromatography (HPLC) analysis of AG1478, AG-1557 showed high and stable recoveries (>86%) from mouse plasma after protein precipitation extraction with cold acetonitrile containing 50 µM internal standard. The relative standard deviation (RSD) of AG-1557 recovery in multiple samples was 4.3%. [2] The 10 mM dimethyl sulfoxide (DMSO) stock solution of AG-1557 remained stable after storage at -70°C for at least 3 months. After dilution in acetonitrile-water solution (1:200), the injection results showed stable peak areas with less than 9% relative standard deviation (RSD) between batches over 3 months. [2]
When 50 µM of an aqueous solution of AG-1557 (acetonitrile-water solution) was repeatedly injected into the high-performance liquid chromatography (HPLC) system over 32 hours (more than 40 injections), the peak area remained stable, and no cross-contamination between injections was found, indicating that the compound has good stability in the autosampler under analytical conditions. [2] |
| References |
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| Additional Infomation |
AG-1557 (4-(3-iodoanilino)-6,7-dimethoxyquinazoline) was used as an internal standard in a high-performance liquid chromatography (HPLC) method for the analysis of typhoid salmonella AG1478 in mouse plasma. [2] AG-1557 was chosen as the internal standard because it is a quinazoline analog with a structure similar to the analyte (AG1478), elutes after the analyte under the chromatographic conditions, exhibits similar extraction characteristics, and demonstrates excellent stability in the autosampler throughout the analytical run. [2] The chromatographic method employed a reversed-phase C8 column with gradient elution using acetonitrile/ammonium acetate buffer. Under these conditions, AG-1557 eluted as a single symmetrical peak with a retention time of 32.5 min, later than the retention time of AG1478 (31.4 min). [2]
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| Molecular Formula |
C16H14IN3O2
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|---|---|---|
| Molecular Weight |
407.21
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| Exact Mass |
407.013
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| Elemental Analysis |
C, 47.19; H, 3.47; I, 31.16; N, 10.32; O, 7.86
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| CAS # |
189290-58-2
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| Related CAS # |
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| PubChem CID |
5328201
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| Appearance |
Off-white to gray solid powder
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| Density |
1.7±0.1 g/cm3
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| Boiling Point |
492.9±45.0 °C at 760 mmHg
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| Flash Point |
251.9±28.7 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.708
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| LogP |
4.34
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
22
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| Complexity |
360
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=CC(=C3)I)OC
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| InChi Key |
FGCLAQLIXMAIHT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H14IN3O2/c1-21-14-7-12-13(8-15(14)22-2)18-9-19-16(12)20-11-5-3-4-10(17)6-11/h3-9H,1-2H3,(H,18,19,20)
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| Chemical Name |
N-(3-iodophenyl)-6,7-dimethoxyquinazolin-4-amine
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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: ≥ 2.08 mg/mL (5.11 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 (5.11 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 (5.11 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 | 2.4557 mL | 12.2787 mL | 24.5574 mL | |
| 5 mM | 0.4911 mL | 2.4557 mL | 4.9115 mL | |
| 10 mM | 0.2456 mL | 1.2279 mL | 2.4557 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.
Products are for research use only; We do not sell to patients
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