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Pelitinib (EKB-569)

EGFR inhibitor,potent and irreversible CAS# 257933-82-7

Pelitinib (EKB-569)

Catalog No. BCC1118----Order now to get a substantial discount!

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Chemical structure

Pelitinib (EKB-569)

3D structure

Chemical Properties of Pelitinib (EKB-569)

Cas No. 257933-82-7 SDF Download SDF
PubChem ID 6445562 Appearance Powder
Formula C24H23ClFN5O2 M.Wt 467.92
Type of Compound N/A Storage Desiccate at -20°C
Synonyms EKB-569; WAY-EKB 569
Solubility DMSO : 25 mg/mL (53.43 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
Chemical Name (E)-N-[4-(3-chloro-4-fluoroanilino)-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide
SMILES CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)F)Cl)C#N)NC(=O)C=CCN(C)C
Standard InChIKey WVUNYSQLFKLYNI-AATRIKPKSA-N
Standard InChI InChI=1S/C24H23ClFN5O2/c1-4-33-22-12-20-17(11-21(22)30-23(32)6-5-9-31(2)3)24(15(13-27)14-28-20)29-16-7-8-19(26)18(25)10-16/h5-8,10-12,14H,4,9H2,1-3H3,(H,28,29)(H,30,32)/b6-5+
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Pelitinib (EKB-569)

DescriptionPelitinib is a potent irreversible inhibitor of EGFR with IC50 value of 38.5 nM.
TargetsEGFR    
IC5038.5 nM     

Protocol

Cell Assay [1]
For experiments using cells in culture, A431 cells or 3T3/c-erbB-2 cells over-expressing c-erbB2 are are treated with various concentrations of EKB-569 for 2.75 h before co-incubation with 100 ng/mL EGF (A431 cells) or no growth factor (3T3/c-erbB-2 cells) for 0.25 h. Cells are ished twice with cold phosphate-buffered saline (PBS) before adding to lysis buffer for 20 min on ice, before immunoprecipitation and SDS–PAGE-immunoblotting[1].

Animal Administration [1]
Mice: For in vivo experiments, athymic nu/nu female mice are implanted subcutaneously with 5×106 A431 tumor cells. When tumors reach a mass of 200-300 mg, animals are treated with a single dose of 10 mg/kg EKB-569 in pH 2.0 water per gavage. Tumors from control and drug-treated animals are excised and minced into 1-mm pieces for anlysis[1].

References:
[1]. Torrance CJ, et al. Combinatorial chemoprevention of intestinal neoplasia. Nat Med. 2000 Sep;6(9):1024-8. [2]. Nunes M, et al. 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.

Pelitinib (EKB-569) Dilution Calculator

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Preparing Stock Solutions of Pelitinib (EKB-569)

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.1371 mL 10.6856 mL 21.3712 mL 42.7423 mL 53.4279 mL
5 mM 0.4274 mL 2.1371 mL 4.2742 mL 8.5485 mL 10.6856 mL
10 mM 0.2137 mL 1.0686 mL 2.1371 mL 4.2742 mL 5.3428 mL
50 mM 0.0427 mL 0.2137 mL 0.4274 mL 0.8548 mL 1.0686 mL
100 mM 0.0214 mL 0.1069 mL 0.2137 mL 0.4274 mL 0.5343 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Pelitinib (EKB-569)

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.

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References on Pelitinib (EKB-569)

Pelitinib (EKB-569) targets the up-regulation of ABCB1 and ABCG2 induced by hyperthermia to eradicate lung cancer.[Pubmed:25988710]

Br J Pharmacol. 2015 Aug;172(16):4089-106.

BACKGROUND AND PURPOSE: Pelitinib is a potent irreversible EGFR TK inhibitor currently in clinical trials for the treatment of lung cancer. Hyperthermia has been applied concomitantly with chemotherapy and radiotherapy to enhance treatment outcome. In this study, we investigated the ability of the combination of pelitinib with other conventional anticancer drugs to specifically target cancer cells with up-regulated efflux transporters ABCB1/ABCG2 after hyperthermia as a novel way to eradicate the cancer stem-like cells responsible for cancer recurrence. EXPERIMENTAL APPROACH: Alterations in intracellular topotecan accumulation, the efflux of fluorescent probe substrates, expression and ATPase activity of ABCB1/ABCG2 and tumoursphere formation capacity of side population (SP) cells sorted after hyperthermia were examined to elucidate the mechanism of pelitinib-induced chemosensitization. KEY RESULTS: While pelitinib did not modulate ABCB1/ABCG2 expressions, the combination of pelitinib with transporter substrate anticancer drugs induced more marked apoptosis, specifically in cells exposed to hyperthermia. The flow cytometric assay showed that both ABCB1- and ABCG2-mediated drug effluxes were significantly inhibited by pelitinib in a concentration-dependent manner. The inhibition kinetics suggested that pelitinib is a competitive inhibitor of ABCB1/ABCG2, which is consistent with its ability to stimulate their ATPase activity. SP cells sorted after hyperthermia were found to be more resistant to anticancer drugs, presumably due to the up-regulation of ABCB1 and ABCG2. Importantly, pelitinib specifically enhanced the chemosensitivity but reduced the tumoursphere formation capacity of these SP cells. CONCLUSIONS AND IMPLICATIONS: This study demonstrated a novel approach, exploiting drug resistance, to selectively kill cancer stem-like cells after hyperthermia.

Description

Pelitinib (EKB-569;WAY-EKB 569) is an irreversible inhibitor of EGFR with an IC50 of 38.5 nM; also slightly inhibits Src, MEK/ERK and ErbB2 with IC50s of 282, 800, and 1255 nM, respectively.

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