Pelitinib New

Data Sheet For research use only. Not for human use.

Cat. No. ：BCP02376CAS No. ：257933-82-7Purity：98%

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CAS No.	257933-82-7	Cat. No.	BCP02376
Name	Pelitinib
Synonyms	EKB-569;WAY-EKB 569;EKB569;EKB 569; WAY-172569; WAY 172569; WAY172569;
SMILES	O=C(NC1=C(OCC)C=C2N=CC(C#N)=C(NC3=CC=C(F)C(Cl)=C3)C2=C1)/C=C/CN(C)C
Chemical Name
Formula	C24H23ClFN5O2	M. Wt	467.92
Purity	98%	Storage	Store at 4-8°C
Description	Pelitinib displays much higher inhibitory activity against EGFR, compared with the closely related c-erbB-2, as well as other kinases such as Src, Cdk4, c-Met, Raf, and MEK/ERK, with IC50 ranging from 282 nM for Src to >20 μM for Cdk4. Consistently, Pelitinib treatment significantly inhibits the autophosphorylation of EGFR but not c-Met in A431 cells.Pelitinib potently inhibits the proliferation of normal human keratinocytes (NHEK), as well as A431 and MDA-468 tumor cells with IC50 of 61 nM, 125 nM, and 260 nM, respectively, while displaying little activity against MCF-7 cells with IC50 of 3.6 μM. Pelitinib inhibits EGF-induced phosphorylation of EGFR in A431 and NHEK cells with IC50 of 20-80 nM, as well as the phosphorylation of STAT3 with IC50 of 30-70 nM. Pelitinib at 75-500 nM also specifically inhibits the activation of AKT and ERK1/2, without affecting NF-κB pathway.