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Pelitinib

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.

Product Specifications

CAS Number

[257933-82-7]

Product Name Alternative

EKB-569; WAY-EKB 569

UNSPSC

12352005

Hazard Statement

H301

Target

EGFR; Src

Type

Reference compound

Related Pathways

JAK/STAT Signaling; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Pelitinib.html

Purity

99.13

Solubility

DMSO : 25 mg/mL (ultrasonic)

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

Molecular Formula

C24H23ClFN5O2

Molecular Weight

467.92

Precautions

H301

References & Citations

[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.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 2

Isoform

EGFR/ErbB1/HER1

Available Sizes

Curated Selection

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