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AG-1478
🥰Excellent
Catalog No. T2047Cas No. 153436-53-4
Alias Tyrphostin AG-1478, NSC 693255, AG1478
AG-1478 (NSC-693255) (Tyrphostin AG-1478) is a selective EGFR inhibitor.
AG-1478
🥰Excellent
Purity: 99.71%
Catalog No. T2047Alias Tyrphostin AG-1478, NSC 693255, AG1478Cas No. 153436-53-4
AG-1478 (NSC-693255) (Tyrphostin AG-1478) is a selective EGFR inhibitor.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 5 mg | $45 | In Stock | |
| 10 mg | $61 | In Stock | |
| 25 mg | $114 | In Stock | |
| 50 mg | $207 | In Stock | |
| 100 mg | $288 | In Stock | |
| 200 mg | $374 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $50 | In Stock |
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Purity:99.71%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | AG-1478 (NSC-693255) (Tyrphostin AG-1478) is a selective EGFR inhibitor. |
| Targets&IC50 | EGFR:3 nM |
| In vitro | Co-administration of 0.4 mg AG-1478 with a single dose of 25 μCi 90Y-CHX-A''-DTPA-hu3S193 results in significantly enhanced potency compared to the drugs administered separately. AG-1478 blocks phosphorylation of EGFR at tumor sites and inhibits growth in xenograft models of A431 cells overexpressing wt EGFR and glioma expressing de2-7 EGFR. Even subtherapeutic doses of AG-1478 significantly increase the potency of cytotoxic drugs. The combination of AG-1478 and temozolomide shows synergistic antitumor activity against human glioma xenografts. |
| In vivo | At a concentration of 0.25 μM, AG-1478 effectively inhibits Ang II, Ca2+ ionophore, and EGF-induced MAPK activation in VSMCs, without affecting fosinopril or platelet-derived growth factor-BB (PDGF-BB)-induced MAPK activation. AG-1478 also suppresses EGF-induced mitosis in BaF/ERX and LIM1215 cells, with IC50 values of 0.07 μM and 0.2 μM, respectively. Furthermore, AG-1478 inhibits the function of ABC (ATP-binding cassette) transport proteins, such as ABCB1 and ABCG2, showing a more significant effect on ABCG2. In comparison to cells expressing endogenous wild-type EGFR or overexpressing exogenous wild-type EGFR (with IC50 values of 34.6 μM and 48.4 μM respectively), AG-1478 preferentially inhibits U87 mg cells expressing ΔEGFR, with an IC50 of 8.7 μM. It also preferentially inhibits tyrosine kinase activity and autophosphorylation of ΔEGFR over endogenous or overexpressed exogenous wild-type EGFR. |
| Cell Research | Cells are exposed to different concentrations of AG-1478 for 72 hours in 96-well plates. The effects of AG-1478 on cell growth are examined using an Alamar Blue assay. A 20-μL aliquot of Alamar Blue is added to each well, and its absorbance is determined using a Spectromax Scanning Micro plate Reader. The effects of AG-1478 are expressed as percentage of growth inhibition using untreated cells as the control (0% inhibition). Cellular DNA synthesis is determined using a [3H]thymidine incorporation assay. (Only for Reference) |
| Alias | Tyrphostin AG-1478, NSC 693255, AG1478 |
| Molecular Weight | 315.75 |
| Formula | C16H14ClN3O2 |
| Cas No. | 153436-53-4 |
| Smiles | N(C=1C2=C(C=C(OC)C(OC)=C2)N=CN1)C3=CC(Cl)=CC=C3 |
| Relative Density. | 1.337g/cm3 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
| Solubility Information | Ethanol: < 1 mg/mL  H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 4.23 mg/mL (13.4 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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Keywords
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