|Description||Butein, a plant polyphenol isolated from Rhus verniciflua, is able to inhibit the activation of protein tyrosine kinase, NF-κB and STAT3, also inhibits EGFR. The use of these compounds in the treatment of breast cancer on the estrogen ground has been taken into account.|
CGP-59326, a pyrrolopyrimidine derivative, has been found to be an EGFR antagonist and could used in antineoplastic studies.
XL647 is an orally bioavailable small-molecule receptor tyrosine kinase inhibitor with potential antineoplastic activity. It inhibits EGFR, HER2, VEGFR and EphB...
Irbinitinib,also known as ARRY-380 and ONT-380, is an orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (also...
Sapitinib, also known as AZD-8931, is an erbB receptor tyrosine kinase inhibitor with potential antineoplastic activity. AZD8931 binds to and inhibits erbB tyro...
AG 555 is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (IC50 = 0.7 μM) with 50-fold and >140-fold selectivity over ErbB2 and insulin rec...
Tarloxotinib bromide, a pyridopyrimidine derivative, has been found to be a EGFR tyrosine kinase inhibitor precursor and could probably be effective in antineop...
AG-1478 (NSC 693255) is a selective EGFR inhibitor with IC50 of 3 nM; almost no activity on HER2-Neu, PDGFR, Trk, Bcr-Abl and InsR.
BGB-283 is a selective Epidermal growth factor receptor and Proto oncogene protein b raf inhibitor under the development of BeiGene. BGB-283 shows antitumor act...
AST-1306 functions as an irreversible inhibitor, most likely through covalent interaction with Cys797 and Cys805 in the catalytic domains of EGFR and ErbB2, res...
PD153035 is a ATP-competitive EGFR inhibitor with an IC50 and Ki of 25 and 6 pM. PD153035 effectively blocks the enhancement of mitogenesis, induction of early ...
OSI-420 (CP-473420) is an active metabolite of erlotinib which is an orally active EGFR tyrosin kinase inhibitor with IC50 of 2 and 20 nM for the inhibition of ...
MP-412 (AV-412) is a second-generation, orally bioavailable dual kinase inhibitor with potential antineoplastic activity. EGFR/HER2 inhibitor AV-412 binds to an...
Icotinib Hydrochloride (BPI-2009H), or Icotinib, is a highly selective, first generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI).
Erlotinib HCl potently inhibits EGFR activation in intact cells including HNS human head and neck tumor cells (IC50 20nM), DiFi humancolon cancer cells andMDA M...
Mutant EGFR inhibitor
Naquotinib is a irreversible, third-generation, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activitywith ...
PD153035 is a potent and specific inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM; little effect noted against PGDFR, FGFR, CSF-1, InsR and Src.
AG 18 (10 μM) inhibits EGF-induced proliferation of GH3 cells.
Mubritinib, also known as TAK-165, is a protein kinase inhibitor which was under development by Takeda for the treatment of cancer. It completed phase I clinic...
AST-1306 is a novel irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, also effective in mutation EGFR T790M/L858R, more potent to ErbB2-ove...