Home>>Signaling Pathways>> JAK/STAT Signaling>> EGFR>>AG-1557

AG-1557 (Synonyms: Tyrphostin AG-1557)

Catalog No.GC12864

inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase

Products are for research use only. Not for human use. We do not sell to patients.

AG-1557 Chemical Structure

Cas No.: 189290-58-2

Size Price Stock Qty
5mg
$52.00
In stock
10mg
$81.00
In stock
25mg
$153.00
In stock
50mg
$255.00
In stock

Tel:(909) 407-4943 Email: sales@glpbio.com

Customer Reviews

Based on customer reviews.

  • GlpBio Citations

    GlpBio Citations
  • Bioactive Compounds Premium Provider

    Bioactive Compounds Premium Provider

Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

View current batch:

Background

pIC50: 8.194

AG-1557 is an inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase.

The epidermal growth factor receptor (EGFR) is a member of the receptor family of tyrosine kinases. Receptor tyrosine kinases are involved in various cancer cell behaviors, such as growth, invasion and blood vessel formation. EGFR is found to be over-expressed in several human solid tumors. Thus, EGFR has received much attention as a target for anticancer drugs.

In vitro: A pharmacophore model was developed using a dataset of 77 chemically diverse EGFR inhibitors including AG-1557 using PHASE. Statistically valid Three Dimensional Quantitative Structure Activity Relationship (3D-QSAR) equations were generated. Docking of the probable hits into the crystal structure of EGFR was used as a second filter. Calculation of ADME properties of the probable hits arising out of docking further reduced the number of hits. The pharmacophore results indicated that the presence of two aromatic ring features, one acceptor feature, one donor feature and one hydrophobic feature were necessary for potent inhibitory activity. The generated pharmacophore resulted in a 3D-QSAR model, with a correlation coefficient r2 of 0.9905 and q2 of 0.8764. Docking studies as a second filter reduced the hits to 8. Application of drug-likeness as a third filter gave 6 leads. AG-1557 was screening as an inhibitor of EGFR tyrosine kinase with a predicted pIC50 value of 8.62, which was comparable with its experimental determined value of 8.194 [1].

In vivo: Up to now, there is no animal in vivo data reported.

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Joshi, A. ,Gadhwal, M., and Joshi, U.J. Indentification of potential novel EGFR inhibitors using a combination of pharmacophore and docking methods. Int. J. Pharm. Pharmaceut. Sci. 7(6), (2015).

Chemical Properties

Cas No. 189290-58-2 SDF
Synonyms Tyrphostin AG-1557
Chemical Name N-(3-iodophenyl)-6,7-dimethoxy-4-quinazolinamine
Canonical SMILES IC1=CC(NC2=NC=NC3=CC(OC)=C(OC)C=C32)=CC=C1
Formula C16H14IN3O2 M.Wt 407.2
Solubility ≤0.5mg/ml in ethanol;1.5mg/ml in DMSO;1mg/ml in dimethyl formamide Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.4558 mL 12.279 mL 24.558 mL
5 mM 0.4912 mL 2.4558 mL 4.9116 mL
10 mM 0.2456 mL 1.2279 mL 2.4558 mL
  • Molarity Calculator

  • Dilution Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
**When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / CoA (available online).

Calculate

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

Review for AG-1557

Average Rating: 5 ★★★★★ (Based on Reviews and 27 reference(s) in Google Scholar.)

5 Star
100%
4 Star
0%
3 Star
0%
2 Star
0%
1 Star
0%
Review for AG-1557

GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.

Required fields are marked with *

You may receive emails regarding this submission. Any emails will include the ability to opt-out of future communications.