|Description||Neratinib, also known as HKI-272 or PB272, is an orally available, 6,7-disubstituted-4-anilinoquinoline-3-carbonitrile irreversible inhibitor of the HER-2 receptor tyrosine kinase with potential antineoplastic activity. Neratinib binds to the HER-2 receptor irreversibly, thereby reducing autophosphorylation in cells, apparently by targeting a cysteine residue in the ATP-binding pocket of the receptor. Treatment of cells with this agent results in inhibition of downstream signal transduction events and cell cycle regulatory pathways; arrest at the G1-S (Gap 1/DNA synthesis)-phase transition of the cell division cycle; and ultimately decreased cellular proliferation. Neratinib also inhibits the epidermal growth factor receptor (EGFR) kinase and the proliferation of EGFR-dependent cells.|
|Synonyms||HKI-272; HKI 272; HKI272; PB-272; PB 272; PB 272.|
|Current Developer||Wyeth Inc.|
EGF816 mesylate is the mesylate salt of EGF816 which is a covalent mutant-selective EGFR inhibitor and potently inhibits the T790M.
Selatinib is a Epidermal growth factor receptor(EGFR) and ERbB-2 receptor antagonist as an analog of the quinazoline lapatinib with potential antineoplastic act...
AEE-788 is an orally bioavailable multiple-receptor tyrosine kinase inhibitor. AEE788 inhibits phosphorylation of the tyrosine kinases of epidermal growth facto...
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 ...
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. Th...
BMS-599626 Hydrochloride is a selective and efficacious orally bioavailable inhibitor of the HER1, HER2 and HER4 tyrosine kinases with potential antineoplastic ...
Naquotinib is irreversible, third-generation, epidermal growth factor receptor (EGFR) inhibitor with IC50 value of 70 nM for NCI-H1650 cell growth. It can coval...
AC480, also known as BMS-599626, is an orally bioavailable inhibitor of the HER1, HER2 and HER4 tyrosine kinases (IC50 =22, 32 and 190 nM, respectively) with po...
Icotinib Hydrochloride (BPI-2009H), or Icotinib, is a highly selective, first generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI).
AZ5104, the demethylated metabolite of AZD-9291, is a potent EGFR inhibitor with IC50 of
AG 18 (10 μM) inhibits EGF-induced proliferation of GH3 cells.
Falnidamol, also known as BIBX 1382, is a pyrimido-pyrimidine with antitumor activity. BIBX 1382 inhibits the intracellular tyrosine kinase domain of the Epider...
Lapatinib, used in the form of Lapatinib Ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM, respectively.
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...
AZD-9291 is a third-generation EGFR inhibitor, showed promise in preclinical studies and provides hope for patients with advanced lung cancers that have become ...
TPC-064 is a novel mutant-selective inhibitor of EGFR, which plays a role in NSCLC and therefore becomes a key target for cancer therapy. TPC-064 can selectivel...
PD158780 is a potent, cell-permeable, reversible ATP-competitive inhibitor of EGFR tyrosine kinase activity with IC50 values of 0.008, 49 and 52 nM for EGFR, Er...
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...