EGFR Inhibitor

mRNA synthesis
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.

Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
EGFR inhibitor is a cell permeable, pyrimidine compound that selectively inhibits the EGFR kinase with IC50 value of 21 nM [1].
EGFR is a transmembrane protein, and is a receptor for members of epidermal growth factor family. The binding of EGFR with its ligands induces receptor dimerization and tyrosine autophosphorylation, and leads to cell proliferation. The overactivity of EGFR tyrosine kinases is associated with a number of cancers, inhibition of EGFR can downregulate antiapoptotic proteins such as surviving and upregulate proapoptotic proteins such as Bim. Thus, EGFR inhibitor can induce cell apoptosis, resulting in anti-tumor effectivity [2].
EGFR inhibitor inhibited EGFR kinase in vitro and blocks receptor autophosphorylation in cells. EGFR inhibitor also inhibited L858R and L861Q EGFR mutants with IC50 values of 63 and 4 nM, respectively [1].
References:
1. Q. Zhang, Y. Liu, F. Gao, et al. Discovery of EGFR selective 4,6-disubstituted pyrimidines from a combinatorial kinase-directed heterocycle library. Journal of the American Chemical Society 128(7), 2182-2183 (2006).
2. F. Ciardiello, G. Tortora. EGFR antagonists in cancer treatment. New England Journal of Medicine 358(11), 1160-1174 (2008).
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 413.4 |
Cas No. | 879127-07-8 |
Formula | C21H18F3N5O |
Synonyms | Epidermal Growth Factor Receptor Inhibitor |
Solubility | insoluble in H2O; insoluble in EtOH; ≥60.7 mg/mL in DMSO |
Chemical Name | N-[3-[[6-[[3-(trifluoromethyl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]-cyclopropanecarboxamide |
SDF | Download SDF |
Canonical SMILES | O=C(C1CC1)NC2=CC=CC(NC3=CC(NC4=CC(C(F)(F)F)=CC=C4)=NC=N3)=C2 |
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. |
Quality Control & MSDS
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Chemical structure
