Pelitinib (EKB-569) is a potent, irreversible EGFR inhibitor with an IC50 of 38.5 nM. Pelitinib (EKB-569) also slightly inhibited Src, MEK/ERK, and ErbB2, corresponding to IC50 values of 282 nM, 800 nM, and 1255 nM, respectively. Phase2.

 

Brand: BCM

 

Target: EGFR; Raf; MEK; Src

 

Signaling Pathways: Angiogenesis; JAK/STAT signaling; MAPK; Tyrosine Kinase/Adaptors

 

In Vitro: In an A431 xenograft model with EGFR,Pelitinib (10 mg/kg,p.o.) effectively inhibited EGFR phosphorylation by 90% within 1 h and >50% after 24 h. The mouse airway epithelial cell remodeling model, which can be induced by viral infection, is characterized by delayed but permanent transformation into goblet cell formation. Pelitinib (20 mg/kg/day) can completely block the increase of ciliated cells and the decrease of Clara cells, thus correcting the epithelial cell remodeling in three aspects and significantly inhibiting goblet formation. Pelitinib (20 mg/kg/day) inhibited 87% of tumorigenesis in APCMin/+ mice, similar to the effect of a 2x dose of EKI-785 (40 mg/kg/day), consistent with higher in vivo activity. Pelitinib has a selective inhibitory effect on EGFR signaling in airway epithelial cells.

 

Melting Point: 173-178°C

 

Boiling Point: 655.5±55.0 °C(Predicted)

 

pKa: 12.23±0.43(Predicted)

 

Solubility: Soluble in DMSO. Insoluble in Water; insoluble in Ethanol.

 

GHS: GHS06

 

Isomeric SMILES: CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)F)Cl)C#N)NC(=O)/C=C/CN(C)C  

 

InChIKey: WVUNYSQLFKLYNI-AATRIKPKSA-N  

 

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+ 

 

Attribute
[Chem Name]	(E)-N-[4-(3-chloro-4-fluoroanilino)-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide
[Synonym]	Pelitinib; EKB-569
[CAS No.]	257933-82-7
[EINECS]	803-625-4
[MDL No.]	MFCD09837868
[Formula]	C24H23ClFN5O2
[Molecular]	467.92
[Form]	White to beige powder
[Storage]	Keep in dark place. Inert atmosphere. Store in freezer, under -20°C

Goods Tag