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Pelitinib

Catalog No.: 17022702
Cas No.: 257933-82-7
Purity : 98% 
17022702 - Pelitinib | CAS 257933-82-7

Catalog number : 17022702

CAS number : 257933-82-7

Molecular Formula : C₂₄H₂₃ClFN₅O₂ 

Molecular Weight : 467.92 

Iupac Chemical Name : Pelitinib 

Smile : CCOc1cc2c(cc1NC(=O)/C=C/CN(C)C)c(c(cn2)C#N)Nc3ccc(c(c3)Cl)F

InChiKey : WVUNYSQLFKLYNI-AATRIKPKSA-N

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SynonymsEKB-569; WAY-EKB 569; EKB569; EKB 569 
Molecular FormulaC₂₄H₂₃ClFN₅O₂ 
Molecular Weight467.92 
Appearanceoff-white solid 
Purity98% 
SolubilitySoluble in DMSO 
Storage3 years -20ºCpowder 
Shipping ConditionShipped under ambient temperature as non-hazardous chemical. 
SmileCCOc1cc2c(cc1NC(=O)/C=C/CN(C)C)c(c(cn2)C#N)Nc3ccc(c(c3)Cl)F
InChiKeyWVUNYSQLFKLYNI-AATRIKPKSA-N
InChiInChI=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+
MDLMFCD09837868
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Pelitinib (EKB-569; WAY-EKB 569) is a potent irreversible EGFR inhibitor with IC50 of 38.5 nM.

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 M for Cdk4. Consistently, Pelitinib treatment significantly inhibits the autophosphorylation of EGFR but not c-Met in A431 cells [1]. 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 M. 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-B pathway. In NHEK cells, Pelitinib also potently inhibits TGF- mediated EGFR activation with IC50 of 56 nM, as well as activation of STAT3 and ERK1/2 with IC50 of 60 nM and 62 nM, respectively 

 

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