Epidermal Growth Factor Receptor (EGFR)

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PZ0129 CP-380736 ≥98% (HPLC) CP-380736 is an inhibitor of the epidermal growth factor receptor (EGFR). EGFR is a tyrosine kinase that activates MAPK, JNK, and Akt pathways, and is an important mediator of several types of cancer, including lung cancer and glioblastoma multiforme.
SML1657 Gefitinib ≥98% (HPLC) Gefitinib is a selective epidermal growth factor receptor tyrosine kinase (EGFR TK) inhibitor. Gefitinib has antineoplastic activity, and has been approved for the treatment on non-small cell lung cancer (NSCLC).
SML1312 Mubritinib ≥98% (HPLC) Mubritinib (TAK-165) is a potent and selective inhibitor of the human epidermal growth factor receptor 2 ErbB (HER2) tyrosine kinase. Mubritinib potently inhibits proliferation of cancer cell lines over- expressing ErbB2.
SML0564 PD153035 hydrochloride ≥98% (HPLC) PD153035 is apotent and selective ATP competitive inhibitor of the epidermal growth factor receptor tyrosine kinase EGFR.
PZ0285 PD168393 ≥98% (HPLC) PD168393 is potent, cell-permeable, irreversible and selective inhibitor of EGF receptor (EGFR) tyrosine kinase and ErbB2. PD168393 has an IC50 value of 0.70 nM for EGFR, and is inactive against insulin, PDGFR, FGFR and PKC.
PZ0197 Pelitinib ≥98% (HPLC) Pelitinib (EKB-569) is an orally active, potent, second generation irreversible epidermal growth factor receptor tyrosine kinase (EGFR TK) inhibitor. Pelitinib is selective for EGFR (ErbB-1) with an IC50 about 80 nM, but also covalently binds to ErbB-2 (HER2/c-neu) and ErbB-4 (Her 4) with much lower potency. Pelitinib has been shown to inhibit the growth of EGFR-overexpressing tumor cell lines.
PZ0296 PF-06459988 ≥98% (HPLC) PF-06459988 is an orally available irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant (EGFRm) forms including the secondary acquired resistance mutation T790M. PF-06459988 has minimal activity against wild-type EGFR (WT EGFR).
PZ0243 PF-06672131 ≥95% (HPLC) PF-06672131 is a selective EGFR kinase inhibitor thought to covalently react with active-site cysteine residues in the ATP binding pocket. PF-06672131 has been used as a probe for proteomic analysis to identify off-target binding substrates. The dimethylaminomethyl (DMAM) group appears to increase compound stability in cancer cells with a resultant increase in protein reactivity from selective EGFR binding to widespread proteome-wide reactivity after treatment.
PZ0342 PF-6274484 ≥98% (HPLC) PF-6274484 is an irreversible EGFR kinase inhibitor that covalently reacts with active-site cysteine residues in the ATP binding pocket. PF-6274484 inhibits autophosphorylation of both wild type and mutant EGFR in tumor cells with IC50 values of 5.8 nM and 6.6 nM, respectively.
PZ0241 PF-6422899 ≥98% (HPLC) PF-6422899 is an alkynylated derivative of PF-6274484; irreversible inhibitor of EGFR kinase activity. PF-6422899 binds covalently to active-site cysteine residues in the ATP binding pocket of EGFR.
SML1095 PKI-166 ≥98% (HPLC) PKI-166 is a potent, selective and orally available EGF-R tyrosine kinase inhibitor. PKI-166 potently inhibits the growth and metastasis of many human cancers including human pancreatic cancer.
R0654 Reveromycin A ≥98% (HPLC), solid Reveromycin A is a polyketide antibiotic from Streptomyces sp. Epidermal growth factor (EGF) inhibitor; apoptosis inducer; G1 phase cell cycle inhibitor having antiproliferative behavior against human cell lines KB and K562 as well as antifungal activity.
T7040 Tyrphostin 1 ≥98% EGFR tyrosine kinase inhibitor.
Tyrphostin 1 is a small molecule inhibitor of epidermal growth factor (EGF) receptor kinase function. This molecule associates with the substrate subsite of the protein tyrosine kinase (PTK) domain. Tyrphostin 1 is also known to block EGF-dependent receptor autophosphorylation,. Furthermore, studies have reported that tyrphostin 1 can block Ca2+ channels and inhibit growth in vascular smooth muscle cells,.
T7165 Tyrphostin 23 ≥98% Tyrphostin 23 is a small molecule inhibitor of epidermal growth factor (EGF) receptor kinase function. This molecule associates with the substrate subsite of the protein tyrosine kinase (PTK) domain,.
T7665 Tyrphostin 51 ≥98% EGFR tyrosine kinase inhibitor.
Tyrphostin 23 is a small molecule inhibitor of epidermal growth factor (EGF) receptor kinase function. This molecule associates with the substrate subsite of the protein tyrosine kinase (PTK) domain,.
T5068 Tyrphostin AG 658 ≥98%, solid EGFR protein tyrosine kinase inhibitor.
T5443 Tyrphostin AG 825 ≥92.5% EGF receptor tyrosine kinase inhibitor, inactive against IGF-1 Receptor.
Tyrphostin AG 825 has been used in combination with hypericin-mediated photodynamic therapy (HY-PDT) for evaluating its therapeutic effects in HER2 overexpressing human breast cancer cells. This study reported that AG 825 combination increased the induction of cell death, HER2 degradation and inhibited colony formation in cancer cells2.
T5568 Tyrphostin AG 835 ≥92% Protein tyrosine kinase inhibitor.
T4182 Tyrphostin AG 1478 ≥98% Selective inhibitor of epidermal growth factor receptor protein
Studies in human glioma cell lines (U87MG) have shown that tyrphostin AG 1478 preferentially blocks truncated as opposed to the wild-type EGFR4.
T6568 Tyrphostin RG 13022 ≥98% Non-phenolic tyrphostin-class tyrosine kinase inhibitor.
T6693 Tyrphostin RG 14620 ≥98% Non-phenolic tyrphostin-class tyrosine kinase inhibitor.