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Purity: ≥98%
Pelitinib (formerly EKB569; WAY-EKB569; WAY-172569), a 3-cyanoquinoline analog, is an irreversible/covalent EGFR inhibitor with potential antineoplastic activity. It is more selective in inhibiting EGFR than c-Met, Src, erbB-2, Raf, and Cdk4 and has an IC50 of 38.5 nM for the epidermal growth factor receptor (EGFR).
| Targets |
EGFR (IC50 = 38.5 nM); Src (IC50 = 282 nM); MEK/ERK (IC50 = 800 nM); ErbB2 (IC50 = 1.255 μM); Raf (IC50 = 3.353 μM)
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
A431 cells are treated with different concentrations of pelitinib for 2.75 hours prior to co-incubation with 100 ng/mL EGF for 0.25 hours in experiments involving cells in culture. Cold phosphate-buffered saline (PBS) is used to wash cells twice before they are added to lysis buffer (10 mM Tris, pH 7.5, 5 mM ethylenediamine tetra-acetic acid (EDTA), 150 mM NaCl, 1% Triton X-100, 1% Sodium deoxycholate, 0.1% SDS, 1 mM PMSF, 10 mg/mL pepstatin A, 10 mg/mL leupeptin, 20 KIU/mL aprotinin, 2 mM sodium orthovanadate, and 100 mM sodium fluoride). The cells are then left on ice for 20 minutes before being subjected to immunoprecipitation and SDS-PAGE -immunoblotting. Cultured cells are dissolved in cold lysis buffer and then quickly homogenized on ice using a polytron that pulses multiple times in preparation for immunoprecipitation. The mixture is centrifuged twice: once at 2500 rpm for 20 minutes at 4 °C, and once at 14,000 rpm in a microcentrifuge for 10 minutes at 4 °C. Supernatants (1000 μg protein) are incubated with 15 mL of EGFR polyclonal antibody for 2 hours at 4 °C. Following two hours, add 50 μL of protein G plus/protein A agarose beads and incubate at 4 °C for two hours while rotating constantly. Beads are boiled in Laemmli sample buffer for two minutes following washing with lysis buffer. The proteins are then separated using SDS-PAGE, put on an immobilon membrane, and probed using an anti-phosphotyrosine antibody that has been coupled to horseradish peroxidase (HRP) for an overnight period. The ECL reagent is used in the development of membranes. Membrane removal and re-probing with antibodies specific to the receptor yield the total amount of EGFR protein. Densitometry is used to quantify bands, and ImageQuant software along with a Molecular Dynamics laser transmittance scanner are used.
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| Cell Assay |
In 96-well plates, cells are seeded, and after two hours, pelletinib is added. The cells are then incubated for five days. Following incubation, each well's medium is taken out and replaced with 150 μL of fresh medium and 50 μL of a 1 mg/mL MTT solution. Following a 2-hour incubation period at 37 °C, 150 μL of DMSO is added to the medium, and the absorbance at 540 nm in every well is measured. The data are linearly regressed to determine the IC50.
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| Animal Protocol |
Mice: A431 tumor cells measuring 5x106 are subcutaneously inserted into athymic nu/nu female mice for in vivo experiments. Animals receiving treatment receive one gavage of 10 mg/kg EKB-569 in pH 2.0 water when tumor masses approach 200–300 mg. The tumors are removed and chopped into 1-mm pieces for analysis from both drug-treated and control animals[1].
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| References |
| Molecular Formula |
C24H23CLFN5O2
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| Molecular Weight |
467.92
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| Exact Mass |
467.15
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| Elemental Analysis |
C, 61.60; H, 4.95; Cl, 7.58; F, 4.06; N, 14.97; O, 6.84
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| CAS # |
257933-82-7
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| Related CAS # |
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| Appearance |
White to off white powder
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| SMILES |
CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)F)Cl)C#N)NC(=O)/C=C/CN(C)C
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| InChi Key |
WVUNYSQLFKLYNI-AATRIKPKSA-N
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| InChi Code |
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+
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| Chemical Name |
(E)-N-[4-(3-chloro-4-fluoroanilino)-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide
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| Synonyms |
Pelitinib; EKB569; WAY-172569; EKB-569; EKB 569; WAY 172569; WAY172569
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.34 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (5.34 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1371 mL | 10.6856 mL | 21.3712 mL | |
| 5 mM | 0.4274 mL | 2.1371 mL | 4.2742 mL | |
| 10 mM | 0.2137 mL | 1.0686 mL | 2.1371 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00098501 | Completed | Drug: pelitinib Drug: temsirolimus |
Unspecified Adult Solid Tumor, Protocol Specific |
National Cancer Institute (NCI) |
October 2004 | Phase 1 |
| NCT00072748 | Completed | Drug: EKB-569 | Colorectal Neoplasms Colonic Neoplasms |
Wyeth is now a wholly owned subsidiary of Pfizer |
October 2004 | Phase 2 |
| NCT00067548 | Completed | Drug: EKB-569 | Non-Small-Cell Lung Carcinoma Lung Neoplasms |
Wyeth is now a wholly owned subsidiary of Pfizer |
January 2005 | Phase 2 |
Cell surface expression and functional analysis of ABCG2 and ABCB1 in A549 cells with or without hyperthermia (42.5°C) treatment.Br J Pharmacol.2015 Aug;172(16):4089-106. |
Inhibition of ABCB1-, ABCC1- or ABCG2-mediated efflux of fluorescent probe substrate bypelitinibin drug-resistant cells overexpressing the transporters (left panel) or HEK293 cells stably transfected with the three transporters (right panel).Br J Pharmacol.2015 Aug;172(16):4089-106. |
Inhibition kinetics of ABCB1- and ABCG2-mediated topotecan efflux bypelitinib.Br J Pharmacol.2015 Aug;172(16):4089-106. |
 Effect ofpelitinibon the ATPase activity of ABCB1 (top panel) and ABCG2 (bottom panel).Br J Pharmacol.2015 Aug;172(16):4089-106. |
mRNA and cell surface expression of ABCB1 and ABCG2 in A549 after treatment withpelitinib.Br J Pharmacol.2015 Aug;172(16):4089-106. |
elitinibsensitized A549 cells to apoptosis specifically after exposure to hyperthermia.Br J Pharmacol.2015 Aug;172(16):4089-106. |
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