In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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 .
In vivo: Up to now, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
 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).
|Physical Appearance||A crystalline solid|
|Storage||Store at -20°C|
|Solubility||≤0.5mg/ml in ethanol;1.5mg/ml in DMSO;1mg/ml in dimethyl formamide|
|Shipping Condition||Ship with blue ice, or upon other requests.|
|General tips||For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon.|