Pelitinib (EKB-569) Chemical Structure
BIBW2992 (Afatinib, Tomtovok, Tovok) irreversibly inhibits EGFR/HER2 including EGFRwt, EGFR L858R , EGFR L858R/T790M and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM, 14 nM, respectively.
CI-1033 is a potent tyrosine kinase inhibitor of EGFR and erbB2 with IC50 of 1.5 nM and 9.0 nM, respectively.
Erlotinib HCl also known as Tarceva, CP-358774, OSI-774, NSC-718781 is a HCL salt with IC50 of 2 nM for HER1/EGFR TK.
Gefitinib (Iressa) also known as ZD-1839 & Iressa is a novel potent EGFR tyrosine kinase & Akt phosphorylations inhibitor with IC50 of 37, 26 and 57 nM.
Lapatinib Ditosylate (Tyverb, GW-572016, GW-2016) is a potent purified EGFR and ErbB-2 inhibitor with IC50 of 10.2 and 9.8 nM, respectively.
Vandetanib (Zactima) is a VEGFR and EGFR antagonist and a tyrosine kinase inhibitor with IC50 of 60, 90, 40 nM for HUVEC proliferation, PC-9 cells and tyrosine kinase activity, respectively.
BMS-599626 (AC480) is a highly selective pan-HERKinase inhibitor with IC50 of 20 and 30 nM for the inhibition of HER1and HER2, respectively.
PD153035 HCl is an inhibitor of EGFR, competitive with ATP. EGF Receptor: IC50 = 25 pM (Ki = 6 pM)
Inhibitor of the EGFR and ErbB2 with IC50 0.3 and 16 nM respectively.
AG 490 is a potent epidermal growth factor receptor kinase autophosphorylation inhibitor with an IC50 of 100 nM and 56.8 μM for EGFR and JAK, respectively.
Pelitinib (EKB-569) is a 3-cyanoquinoline pan-ErbB tyrosine kinase inhibitor with potential antineoplastic activity. Pelitinib irreversibly binds covalently to epidermal growth factor receptors (EGFR) ErbB-1, -2 and -4, thereby inhibiting receptor phosphorylation and signal transduction and resulting in apoptosis and suppression of proliferation in tumor cells that overexpress these receptors. Pelitinib inhibits EGF-induced phosphorylation of EGF-R and the growth of tumors that overexpress EGF-R in animal models.[1][2]
| Molecular Weight (WM): | 467.92 |
|---|---|
| Formula: | C24H23ClFN5O2 |
| CAS No.: | 257933-82-7 |
| Synonyms: |
WAY-EKB 569
|
| Dissolve in (25°C): | DMSO ≥13mg/mL |
| Water <1mg/mL | |
| Ethanol <1mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
A collection of 864 bioactive compounds
A collection of 481 inhibitors
A collection of 194 kinase inhibitors
A collection of 85 tyrosine kinase inhibitors.
A collection of 426 FDA approved drugs
A collection of 139 natural products
A collection of 40 chemotherapeutic agents
A unique collection of 17 small molecule modulators
A unique collection of 47 small molecule inhibitors
A unique collection of 63 GPCR small molecules
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