Pelitinib (EKB-569)
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.
Pelitinib (also known as EKB-569), a 3-cyanoquinoline, is a potent, and irreversible inhibitor of epidermal growth factor receptor (EGF-R) tyrosine kinase that inhibits the activity of EGF-R with the half maximal inhibition concentration IC50 value of 38.5 nM in vitro [1].
Pelitinib has been found to exert a potent anti-proliferative activity against tumor cells overexpressing EGF-R, including NHEK, A431 and MDA-468 cells, with IC50 values of 61 nM, 125 nM and 260 nM respectively; while it has also been found to potently inhibit EGF-induced phosphorylated EGF-R (pEGF-R) in A431 and NHEK cells with IC50 values ranging from 20 nM to 80 nM [2].
References:
[1] Torrance CJ, Jackson PE, Montgomery E, Kinzler KW, Vogelstein B, Wissner A, Nunes M, Frost P, Discafani CM. Combinatorial chemoprevention of intestinal neoplasia. Nat Med. 2000 Sep;6(9):1024-8.
[2] Nunes M, Shi C, Greenberger LM. Phosphorylation of extracellular signal-regulated kinase 1 and 2, protein kinase B, and signal transducer and activator of transcription 3 are differently inhibited by an epidermal growth factor receptor inhibitor, EKB-569, in tumor cells and normal human keratinocytes. Mol Cancer Ther. 2004 Jan;3(1):21-7.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 467.92 |
| Cas No. | 257933-82-7 |
| Formula | C24H23ClFN5O2 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥11.7 mg/mL in DMSO |
| Chemical Name | (E)-N-[4-(3-chloro-4-fluoroanilino)-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide |
| SDF | Download SDF |
| Canonical SMILES | CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)F)Cl)C#N)NC(=O)C=CCN(C)C |
| 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. |
| Description | Pelitinib is a potent irreversible inhibitor of EGFR with IC50 value of 38.5 nM. | |||||
| Targets | EGFR | |||||
| IC50 | 38.5 nM | |||||
Quality Control & MSDS
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Chemical structure
