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EGFR and HER2 inhibitors act on two closely related receptor tyrosine kinases of the ErbB family. The epidermal growth factor receptor (EGFR, ErbB1) and human epidermal growth factor receptor 2 (HER2, ErbB2) form dimers with each other and with ErbB3 and ErbB4. Receptor activation engages the mitogen-activated protein kinase (MAPK) and phosphoinositide 3-kinase (PI3K) pathways that control cell growth. Activating EGFR mutations in non-small-cell lung cancer have made the receptor a central model in kinase inhibitor research. Gefitinib and erlotinib are reversible EGFR inhibitors, and lapatinib inhibits both EGFR and HER2. Osimertinib binds covalently to EGFR carrying the T790M resistance mutation, and neratinib irreversibly inhibits HER2 and EGFR.
Synonyms: AZD 3759
AZD3759 is an orally available inhibitor of the epidermal growth factor receptor (EGFR). It binds to and inhibits the activity of EGFR as well as certain mutant forms of EGFR.
Synonyms: Hemslecin A
Cucurbitacin IIa is a potent EGFR inhibitor with an IC50 of 1.455 nM, demonstrating effective modulation of the EGFR signaling pathway. This compound induces caspase-3-dependent apoptosis, downregulates survivin expression, and enhances autophagy, while disrupting the actin cytoskeleton and arresting the cell cycle at the G2/M phase. Additionally, Cucurbitacin IIa exhibits anti-inflammatory properties, making it a valuable tool for research into inflammation-related diseases, depression, and various cancers, including non-small cell lung cancer.
Khellin is a furochromone that acts as an inhibitor of the epidermal growth factor receptor (EGFR) with an IC50 of 0.15 µM. It demonstrates significant anti-proliferative activity in vitro, making it a valuable compound for cancer research. Additionally, Khellin exhibits antispasmodic properties and coronary vasodilator effects, further broadening its potential applications in biological studies.
Synonyms: CK-101; RX518
Olafertinib (CK-101, RX518) is an epidermal growth factor receptor (EGFR) inhibitor.
Synonyms: RG-50810; RG-50858; TX 825; Tyrphostin 23; Tyrphostin A23; Tyrphostin AG-18
AG-18 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 35 ,M in the human epidermoid carcinoma cell line A431.
Synonyms: HM61713 hydrochloride; BI 1482694 hydrochloride
Olmutinib hydrochloride is an orally active and irreversible inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. By covalently binding to a cysteine residue in the kinase domain, it effectively disrupts signaling pathways associated with non-small cell lung cancer (NSCLC). This compound is utilized in research to study the mechanisms of EGFR-related oncogenesis as well as potential therapeutic strategies for NSCLC treatment.
EAI045 ia a potent and selective EGFR inhbitor. EAI045 targets selected drug-resistant EGFR mutants but spares the wild-type receptor.
Synonyms: AL3818
Anlotinib is a EGFR inhibitor extracted from patent 2015185012 A1, compound 1,which can be used to treat non-small cell lung cancer.
PD158780 is a very potent inhibitor of EGFR with IC50 of 0.08 nM; pan-specific antagonist of ErbB receptor.
HG-14-10-04 is a potent and specific ALK inhibitor with IC50 of 20 nM.
TX1-85-1 is ErbB3 inhibitor. TX2-121-1 may exert Her3-dependent pharmacology through an allosteric mechanismthereby disrupting interactions between Her3 and other proteins such as Her3 or cMet consistent with results presented here and distinct from conventional kinase inhibitors, which block catalytic function.
Synonyms: ONT-380; Irbinitinib; ARRY-380
ARRY-380 is an orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (also called HER2) with potential antineoplastic activity.
NSC 228155 is an activator of EGFR, binds to the extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR.
Synonyms: AC-0010; Abivertinib
Avitinib (AC0010) is a pyrrolopyrimidine-based irreversible EGFR inhibitor that is mutation-selective with IC50 value of 0.18 nM against EGFR L858R/T790M double mutations, nearly 43-fold greater potency over wild-type EGFR (IC50 value, 7.68 nM). It has comparable anti-tumor activity and tolerated toxicity.
Synonyms: YH 25448; GNS1480
Lazertinib (YH25448,GNS-1480) is a potent, highly mutant-selective and irreversible EGFR-TKI with IC50 values of 1.7 nM, 2 nM, 5 nM, 20.6 nM and 76 nM for Del19/T790M, L858R/T790M, Del19, L85R and Wild type EGFR respectively, showing much higher IC50 values aganist ErbB2 and ErbB4.
Synonyms: SHR-1258 Racemate
Pyrotinib Racemate is the racemate of Pyrotinib. Pyrotinib is a potent and selective EGFR/HER2 dual inhibitor.
Synonyms: Tyrphostin B66
Tyrphostin AG-528, also known as Tyrphostin B66, is a EGFR protein tyrosine kinase inhibitor.
Synonyms: RG-14355; NSC 678027
Lavendustin A is a selective inhibitor of epidermal growth factor (EGF) receptor-associated tyrosine kinase with IC50 value of 11 nM).
Synonyms: Tyrphostin 46; Tyrphostin AG-99; AG99
AG-99 is an epidermal growth factor receptor (EGFR) kinase inhibitor with IC50 value of 10 μM.
Synonyms: Tyrphostin AG-494
AG-494 is an inhibitor of epidermal growth factor receptor kinase with an IC50 value of 1 μM in HT-22 cells.
Synonyms: AZD-9291 mesylate; Mereletinib mesylate
Osimertinib mesylate is a mutant-selective inhibitor of the epidermal growth factor receptor (EGFR), acting through a covalent and irreversible mechanism. It demonstrates potent biological activity with an apparent IC50 of 12 nM against the L858R mutation and 1 nM against the L858R/T790M mutation. Osimertinib mesylate is primarily utilized in research focused on overcoming T790M-mediated resistance to existing EGFR-targeted therapies in lung cancer.
Synonyms: GW572016 ditosylate monohydrate; GW2016 ditosylate monohydrate
Lapatinib ditosylate monohydrate is a selective inhibitor of the ErbB-2 and EGFR tyrosine kinase domains. It demonstrates potent biological activity with IC50 values of 10.2 nM against EGFR and 9.8 nM against ErbB-2. This compound is commonly utilized in cancer research to investigate mechanisms of tumor growth and resistance, particularly in breast cancer models.
Synonyms: AZD-9291; AZD 9291 (dimesylate); Mereletinib (dimesylate)
Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively.
MTX-211 is a dual inhibitor of EGFR and PI3K, which plays important roles in the progression of KRAS mutant colorectal cancer. MTX-211 has the potential for the treatment of KRAS mutant colorectal cancer.
Synonyms: Tyrphostin RG14620
RG14620 is an EGFR inhibitor with an IC50 of 3 μM.
