Art. -Nr.: HY-32718

Pelitinib

(Synonyms: EKB-569; WAY-EKB 569)

10 Cited Publications

Kundenbewertung

Based on 10 publication(s) in Google Scholar

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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Reinheit: 98.52%
CAS. Nr.: 257933-82-7
Formel: C₂₄H₂₃ClFN₅O₂
Molecular Weight:467.92

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Pelitinib Chemical Structure

CAS. Nr.: 257933-82-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (10)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

EGFR

38.5 nM (IC₅₀)

Alle EGFR Isoform-spezifische Produkte anzeigen :

Alle Src Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	0.01 μM Compound: 86 (table 1)	Inhibition of human A431 cell proliferation Inhibition of human A431 cell proliferation	[PMID: 15715478]
A-431	IC₅₀	0.03 μg/mL Compound: 4 (EKB-569)	Inhibition of A431 cell proliferation Inhibition of A431 cell proliferation	[PMID: 12270171]
A-431	IC₅₀	0.08 μM Compound: 5	Concentration required to inhibit growth of human carcinoma epidermoid (A431) cell line Concentration required to inhibit growth of human carcinoma epidermoid (A431) cell line	[PMID: 12502359]
A-431	IC₅₀	8.02 nM Compound: 1,EKB-569	Inhibition of EGFR autophosphorylation in human A431 cells Inhibition of EGFR autophosphorylation in human A431 cells	[PMID: 20797871]
A549	GI₅₀	7.7 μM Compound: 2	Growth inhibition of human A549 cells Growth inhibition of human A549 cells	[PMID: 38870832]
HBL-100	GI₅₀	19 μM Compound: 2	Growth inhibition of human HBL-100 cells Growth inhibition of human HBL-100 cells	[PMID: 38870832]
HeLa	GI₅₀	8.3 μM Compound: 2	Growth inhibition of human HeLa cells Growth inhibition of human HeLa cells	[PMID: 38870832]
Sf9	IC₅₀	38.5 nM Compound: EKB-569	Inhibition of recombinant human His6-tagged EGFR cytoplasmic domain (645 to 1186 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in autophosphorylation preincubated for 10 mins followed by ATP-MgCl2 addition and measured Inhibition of recombinant human His6-tagged EGFR cytoplasmic domain (645 to 1186 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in autophosphorylation preincubated for 10 mins followed by ATP-MgCl2 addition and measured	[PMID: 30600149]
SK-BR-3	IC₅₀	0.007 μg/mL Compound: 4 (EKB-569)	Inhibition of SKBR-3 cell proliferation Inhibition of SKBR-3 cell proliferation	[PMID: 12270171]
SK-BR-3	IC₅₀	0.68 μM Compound: 86 (table 1)	Inhibition of human SKBr3 cell proliferation Inhibition of human SKBr3 cell proliferation	[PMID: 15715478]
SW1573	GI₅₀	20 μM Compound: 2	Growth inhibition of human SW1573 cells Growth inhibition of human SW1573 cells	[PMID: 38870832]
SW-620	IC₅₀	0.317 μg/mL Compound: 4 (EKB-569)	Inhibition of SW-620 cell proliferation Inhibition of SW-620 cell proliferation	[PMID: 12270171]
SW-620	IC₅₀	0.68 μM Compound: 5	Concentration required to inhibit growth of human carcinoma colon (SW620) cell line Concentration required to inhibit growth of human carcinoma colon (SW620) cell line	[PMID: 12502359]
SW-620	IC₅₀	0.68 μM Compound: 86 (table 1)	Inhibition of human SW620 cell proliferation Inhibition of human SW620 cell proliferation	[PMID: 15715478]
T47D	GI₅₀	16 μM Compound: 2	Growth inhibition of human T47D cells Growth inhibition of human T47D cells	[PMID: 38870832]
Vero C1008	EC₅₀	1.25 μM Compound: pelitinib	Antiviral activity against SARS-COV2 infected in African green monkey Vero E6 cells assessed as reduction of viral titer by immunofocus assay Antiviral activity against SARS-COV2 infected in African green monkey Vero E6 cells assessed as reduction of viral titer by immunofocus assay	[PMID: 36920850]
WiDr	GI₅₀	12 μM Compound: 2	Growth inhibition of human WiDr cells Growth inhibition of human WiDr cells	[PMID: 38870832]

In Vitro

Pelitini has much greater inhibitory activity against the EGFR kinase than against Src, MEK/ERK, Cdk4, c-Met, Raf and ErbB2, for example, the IC₅₀ for EGFR is 32-fold lower than the IC₅₀ for the closely related ErbB2. Pelitinib results in a dramatic reduction in EGFR phosphorylation but no change in the total amount of EGFR protein. It requires at least 10-fold more drug to equivalently inhibit ErbB2 phosphorylation in similar assays, and EKB-569 does not block phosphorylation of another receptor tyrosine kinase (c-Met) assessed in the same manner^[1].
EKB-569 is a potent inhibitor of proliferation in NHEK, A431, and MDA-468 cells (IC₅₀=61, 125, and 260 nM, respectively) but not MCF-7 cells (IC₅₀=3600 nM). EKB-569 is also a potent inhibitor of EGF-induced phosphorylated EGF-R (pEGF-R) in A431 and NHEK cells (IC₅₀=20-80 nM)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

A single oral dose of 10 mg/kg EKB-569 inhibits EGFR phosphorylation in A431 xenografts within 60 minutes. Twenty-four hours later, EGFR activity is still inhibited by over 50% by this single oral dose. The half-life of EKB-569 in mouse plasma is about 2 hours^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 257933-82-7
Appearance Solid
Molecular Weight 467.92
Formel C₂₄H₂₃ClFN₅O₂
Color White to off-white
SMILES

N#CC1=C(C2=CC(NC(/C=C/CN(C)C)=O)=C(OCC)C=C2N=C1)NC3=CC(Cl)=C(C=C3)F
Synonyms

EKB-569; WAY-EKB 569
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (10)

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Journal Impact Factor

Signal Transduct Target Ther

Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]

2025 Dec 15;10(1):406. PMID: 41392286
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Pharmacol Res

Ceritinib inhibits growth and ACTH production of PitNETs: Insights from patient-derived organoids. [Abstract]

2025 Nov:221:107993. PMID: 41083089
J Pharm Anal

Dissection of triple-negative breast cancer microenvironment and identification of potential therapeutic drugs using single-cell RNA sequencing analysis. [Abstract]

2024 Aug;14(8):100975. PMID: 39263352
Sci Data

High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]

2024 Sep 19;11(1):1024. PMID: 39300112
J Med Chem

Probing Ligand Binding Sites on Large Proteins by Nuclear Magnetic Resonance Spectroscopy of Genetically Encoded Non-Canonical Amino Acids. [Abstract]

2023 Apr 13;66(7):5289-5304. PMID: 36920850
Sci Rep

Emetine dihydrochloride suppresses the invasiveness and motility of hepatocellular carcinoma cells through MAPK pathway inhibition and Twist1 protein destabilization. [Abstract]

2026 Jun 23. PMID: 42337289
bioRxiv

Coupling high-throughput protease enzymology with viral replication reveals biochemical constraints of viral fitness. [Abstract]

2026 Jan 28:2026.01.27.702130. PMID: 41659632
bioRxiv

2025 Nov 17.
Hong Kong Polytechnic University

2025.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 25 mg/mL (53.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.34 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (5.34 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

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

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1371 mL	10.6856 mL	21.3712 mL	53.4279 mL
	5 mM	0.4274 mL	2.1371 mL	4.2742 mL	10.6856 mL
	10 mM	0.2137 mL	1.0686 mL	2.1371 mL	5.3428 mL
	15 mM	0.1425 mL	0.7124 mL	1.4247 mL	3.5619 mL
	20 mM	0.1069 mL	0.5343 mL	1.0686 mL	2.6714 mL
	25 mM	0.0855 mL	0.4274 mL	0.8548 mL	2.1371 mL
	30 mM	0.0712 mL	0.3562 mL	0.7124 mL	1.7809 mL
	40 mM	0.0534 mL	0.2671 mL	0.5343 mL	1.3357 mL
	50 mM	0.0427 mL	0.2137 mL	0.4274 mL	1.0686 mL

Keywords

Pelitinib

10 Cited Publications

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Pelitinib

Immunology/Inflammation Compound Library

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Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Pelitinib

Alle EGFR Isoform-spezifische Produkte anzeigen

Alle Src Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (10)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Pelitinib Related Classifications

HY-32718 Related Classifications