Pelitinib
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
| Packaging | Price | Availability | Purity | Estimated Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry |
| Synonyms | EKB-569; WAY-EKB 569; EKB569; EKB 569 |
|---|---|
| Molecular Formula | C₂₄H₂₃ClFN₅O₂ |
| Molecular Weight | 467.92 |
| Appearance | off-white solid |
| Purity | 98% |
| Solubility | Soluble in DMSO |
| Storage | 3 years -20ºCpowder |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. |
| Smile | CCOc1cc2c(cc1NC(=O)/C=C/CN(C)C)c(c(cn2)C#N)Nc3ccc(c(c3)Cl)F |
| 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+ |
| MDL | MFCD09837868 |
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
