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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.
HG-5-88-01 is an EGFR inhibitor that disrupts epidermal growth factor receptor signaling pathways. It demonstrates notable anti-cancer activity independent of EGFR expression levels, making it a valuable tool for exploring therapeutic resistance mechanisms. This compound is particularly relevant for research in cancer biology and the development of alternative therapies targeting EGFR.
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EGFR-IN-167 is a selective inhibitor of the epidermal growth factor receptor (EGFR), exhibiting an IC50 of 0.19 nM. This compound demonstrates high potency against various EGFR mutants, with IC50 values of 0.109 nM for EGFR (L858R), 0.75 nM for EGFR (C797S), and
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EGFR kinase inhibitor 4 is a bivalent ATP-allosteric inhibitor of the epidermal growth factor receptor (EGFR), demonstrating an IC50 of 1.8 nM specifically for the mutant EGFR variant (LRTMCS). This compound is primarily utilized in research focused on non-small cell lung cancer (NSCLC), providing insights into EGFR-related signaling pathways and therapeutic resistance mechanisms.
HER2-IN-8 is a potent inhibitor of the human epidermal growth factor receptor 2 (HER2). This compound exhibits significant anti-cancer activity, making it a valuable tool for studying malignancies that overexpress HER2. Additionally, HER2-IN-8 can be utilized in inflammation research, providing insights into its role in related pathological conditions.
EGFR-IN-63 is a potent inhibitor of the epidermal growth factor receptor (EGFR), with an IC50 value of 0.096 μM. This compound demonstrates significant anticancer activity, particularly in MCF-7 breast cancer cells, exhibiting an IC50 of 2.49 μM. EGFR-IN-63 is suitable for research applications involving cancer biology and targeted therapies.
EGFR-IN-87 is an EGFR tyrosine kinase inhibitor that demonstrates potent inhibition with IC50 values of 3.1 nM, 1.3 nM, and 7.1 nM for EGFR_d746-750, EGFR_L858R/T790, and wild-type EGFR in A431 cells, respectively. This compound is valuable for investigating EGFR-related signaling pathways and is applicable in cancer research, particularly in the context of targeted therapies for tumors expressing mutated forms of the receptor.
EGFR mutant-IN-2 (Compound D51) is a selective inhibitor targeting the EGFR mutant variants, specifically EGFRL858R/T790M/C797S and EGFRdel19/T790M/C797S, with IC50 values of 14 nM and 62 nM, respectively. This compound demonstrates significant antitumor activity alongside favorable pharmacokinetic properties and in vivo stability, making it a valuable tool for research in cancer therapeutics. Its ability to effectively inhibit challenging EGFR mutations underscores its potential application in studying resistance mechanisms and developing targeted treatments.
AG 1406 is a potent HER2 inhibitor, exhibiting an IC50 of 10.57 μM against the HER2 receptor in BT474 cells, while demonstrating minimal activity against EGFR with an IC50 greater than 50 μM in EGF-3T3 cells. This compound serves as a valuable tool for research focused on HER2-positive cancer models and therapeutic strategies targeting HER2 pathways. AG 1406 is suitable for studies investigating the role of HER2 in tumor progression and resistance mechanisms.
JBJ-04-125-02 is a potent allosteric inhibitor of the epidermal growth factor receptor (EGFR), demonstrating selective activity against mutant forms, particularly EGFRL858R/T790M, with an IC50 of 0.26 nM. This compound effectively inhibits the proliferation of cancer cells and disrupts signaling pathways associated with EGFRL858R/T790M/C797S mutations. JBJ-04-125-02 exhibits significant anti-tumor properties, making it a valuable tool for research in targeted cancer therapies.
SOS1/EGFR-IN-1 is a dual-target inhibitor that specifically targets SOS1 and EGFR, demonstrating IC50 values of 42.13±1.55 nM and 1.01±0.04 nM, respectively. This compound effectively induces apoptosis and G1 phase cell cycle arrest, while reducing angiogenesis and cell migration. SOS1/EGFR-IN-1 exhibits significant antitumor activity in prostate cancer cells, with an IC50 of 0.45±0.03 μM, making it a valuable tool for research in cancer therapies.
4-Methyl erlotinib is a potent and selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. This compound effectively disrupts EGF-mediated tumor cell proliferation by significantly lowering EGFR-specific tyrosine phosphorylation levels. In preclinical studies utilizing a mouse model of human tumor transplantation, 4-Methyl erlotinib exhibited notable and prolonged inhibition of EGFR phosphotyrosine levels, leading to substantial growth inhibition in EGFR-dependent human malignancies.
EGFR/HER2-IN-9 is a potent inhibitor of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2). It demonstrates inhibitory activity with IC50 values of 3.2 nM against EGFR, 8.3 nM against the EGFR T790M mutant, and 14 nM against HER2. This compound is applicable in research focused on targeted cancer therapies, particularly for tumors exhibiting dysregulated EGFR and HER2 signaling pathways.
EGFR-IN-85 is a selective inhibitor of the epidermal growth factor receptor (EGFR), demonstrating an IC50 value of 0.19 μM for EGFRvIII phosphorylation. This compound effectively suppresses EGFR signaling within tumor microenvironments, making it a valuable tool for studying glioblastoma (GBM) and related malignancies. Researchers can utilize EGFR-IN-85 to elucidate the role of EGFR in tumor progression and to explore potential therapeutic interventions.
YS-67 is a highly effective inhibitor of the epidermal growth factor receptor (EGFR), exhibiting an IC50 of 5.2 nM. This compound significantly reduces the phosphorylation of EGFR and AKT, indicating its potential to disrupt downstream signaling pathways. YS-67 demonstrates notable antiproliferative effects on human cancer cell lines, including A549, PC-9, and A431, with IC50 values of 4.1 μM, 0.5 μM, and 2.1 μM, respectively. This makes YS-67 a valuable reagent for research focused on therapeutic strategies targeting EGFR in various cancer models.
EGFR-IN-1 TFA is an irreversible inhibitor targeting the EGFR L858R/T790M mutant, specifically designed to overcome resistance to Gefitinib. It demonstrates exceptional potency, exhibiting a 100-fold selectivity over wild-type EGFR. This compound shows robust antiproliferative effects against H1975 and HCC827 cell lines, highlighting its potential for antitumor applications in the treatment of lung cancer driven by these mutations.
EGFR-IN-69 is a highly selective inhibitor of the epidermal growth factor receptor (EGFR), demonstrating potent activity with IC50 values of 4.3 nM for EGFRL858R/T790M/C797S, 6.6 nM for EGFRL858R/T790M, and 25.6 nM for EGFR19del/T790M/C797S. This compound is particularly relevant for research in non-small-cell lung cancer (NSCLC), providing valuable insights into therapeutic strategies targeting mutant EGFR variants. Its efficacy in inhibiting EGFR activity makes it an important tool for advancing cancer research and drug development.
GW583340 dihydrochloride is a potent dual inhibitor of the epidermal growth factor receptor (EGFR) and ErbB2 tyrosine kinases, with IC50 values of 0.01 μM and 0.014 μM, respectively. This compound effectively reverses drug resistance mediated by ABCG2 and ABCB1 transporters, enhancing the efficacy of chemotherapeutic agents. GW583340 dihydrochloride demonstrates significant anti-cancer activity, making it a valuable tool for research in cancer biology and therapeutic development.
Synonyms: 4,7-DHC
4,7-Dihydroxycoumarin is a potent inhibitor of the epidermal growth factor receptor (EGFR) as well as estrogen and progesterone receptors. It exhibits significant cytotoxicity against breast cancer cells, with an IC50 value of 18.36 μg/mL. This compound is valuable for research focused on breast cancer treatment and the exploration of hormone receptor interactions.
Tyrosine kinase-IN-7 is a selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. It exhibits inhibitory activity with IC50 values of 0.630 μM for EGFR wild-type and 0.956 μM for the T790M mutant variant. Tyrosine kinase-IN-7 demonstrates significant antitumor effects across several cancer cell lines, including HepG2, HCT-116, MCF-7, and A431, with respective IC50 values of 13.02 μM, 10.14 μM, 12.68 μM, and 47.05 μM. This compound is useful for research focused on cancer therapeutics targeting the EGFR signaling pathway.
ES-072 is a selective inhibitor of the EGFR-T790M mutation, primarily targeting this mutant receptor to activate GSK3α. By inhibiting EGFR-T790M activity, ES-072 promotes the phosphorylation of PD-L1 at Ser279 and Ser283, which facilitates its ubiquitination and subsequent proteasomal degradation via the E3 ligase ARIH1. This dual mechanism not only suppresses cancer cell proliferation but also enhances the anti-tumor immune response through reduced PD-L1 expression. ES-072 is applicable in research focused on non-small cell lung cancer (NSCLC) treatment strategies.
BPI-15086 is an orally active, potent, irreversible inhibitor targeting the epidermal growth factor receptor (EGFR) and specifically the T790M resistance mutation. This compound exhibits significant biological activity against mutant EGFR, making it a valuable tool for research focused on non-small-cell lung cancer. Its selective action aids in the study of resistance mechanisms and therapeutic responses associated with EGFR mutations.
Synonyms: ARQ-087 dihydrochloride
Derazantinib dihydrochloride is a potent inhibitor of the fibroblast growth factor receptor (FGFR) family, specifically targeting FGFR1, FGFR2, and FGFR3 with IC50 values of 4.5 nM, 1.8 nM, and 2.4 nM, respectively. Its mechanism involves competitive inhibition of ATP binding, which effectively reduces FGFR phosphorylation. This compound has demonstrated significant anti-tumor effects in various xenograft models, making it valuable for research in cancer biology and targeted therapies.
Synonyms: Xiliertinib tartrate; HMPL-309 tartrate
Theliatinib tartrate is a potent, ATP-competitive inhibitor of the epidermal growth factor receptor (EGFR) with a Ki of 0.05 nM and an IC50 of 3 nM. This compound demonstrates an IC50 of 22 nM for EGFR T790M/L858R mutants and exhibits over 50-fold selectivity for EGFR compared to other kinases. Additionally, Theliatinib tartrate contains an alkyne group, allowing it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it useful for click chemistry applications in research.
JBJ-02-112-05 is a potent allosteric inhibitor of the epidermal growth factor receptor (EGFR), specifically targeting mutant forms such as EGFRL858R/T790M with an IC50 of 15 nM. This compound offers a selective approach to inhibit aberrant EGFR activity, making it valuable for research applications in cancer therapeutics and precision oncology. Its oral bioavailability further enhances its utility in preclinical studies of EGFR-driven tumors.
Synonyms: TAK-788 mesylate; AP32788 mesylate
Mobocertinib mesylate is an orally active and irreversible inhibitor of EGFR and HER2. It exhibits potent inhibition of oncogenic variants with activating EGFR exon 20 insertion mutations while showing selectivity for wild-type EGFR. This reagent is primarily utilized in research focused on non-small cell lung cancer (NSCLC).
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