257933-82-7 Pelitinib AKSci X7489
 
 
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  X7489    
Pelitinib
, 98%
 
EKB-569




IDENTITY
CAS Number:257933-82-7
MDL Number:MFCD09837868
MF:C24H23ClFN5O2
MW:467.92
SPECIFICATIONS & PROPERTIES
Min. Purity Spec:98%
Physical Form (at 20°C):Solid
Melting Point:195-200°C
Long-Term Storage:Store long-term at -20°C
DOT/IATA TRANSPORT INFORMATION
UN #:UN2811
Hazard Class:6.1; Poison
Packing Group:III
A hazmat fee may apply to certain package sizes. Please check pricing table for an indicator of applicable hazmat fees.

BIOLOGICAL INFO
Solubility:DMSO
Application(s):EGFR inhibitor
Form:Free Base
Research Area:Cancer

REVIEW

 Pelitinib (EKB-569; WAY-EKB 569) is a potent irreversible EGFR inhibitor with IC50 of 38.5 nM. IC50 value: 38.5 nM. Target: EGFR in vitro: 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. In NHEK cells, Pelitinib also potently inhibits TGF-a 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. in vivo: A single oral dose of 10 mg/kg Pelitinib potently inhibits the EGFR phosphorylation in A431 xenografts with over-expressed EGFR, by 90% within 1 hour, and by >50% after 24 hours. Administration of Pelitinib at 20 mg/kg/day inhibits tumorigenesis in APCMin/+ mice by 87%, equivalent to the effect of used with 2 times doses of EKI-785 (40 mg/kg/day), consistent with greater in vivo potency. Pelitinib selectively inhibits EGFR signaling in airway epithelial cells in vivo. In the mouse model of airway epithelial remodeling that is inducible by viral infection and features a delayed but permanent switch to goblet cell metaplasia, Pelitinib treatment at 20 mg/kg/day corrects all 3 aspects of epithelial remodeling, by completely blocking the increase of ciliated cells and decrease of Clara cells, and significantly inhibiting the metaplasia of goblet cells.

GLOBALLY HARMONIZED SYSTEM (GHS)

Pictograms

Signal Word
Danger

Hazard Statements
H301

Precautionary Statements
P264; P270; P301+P310; P321; P330; P405; P501


Current as of April 15, 2024


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