Catalog No.
Product Name
Application
Product Information
Citations
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EGFR ADC
Laprituximab emtansine targets the epidermal growth factor receptor (EGFR) as an antibody-drug conjugate (ADC) incorporating the J2898A antibody linked to DM1, an anti-microtubule agent, via the SMCC thioether linker. This compound exhibits potent anti-cancer activity by delivering cytotoxic agents directly to HER1-expressing cells, thereby enhancing therapeutic efficacy while minimizing systemic toxicity. It is suitable for applications in cancer research, particularly in the study of targeted therapies and EGFR-related pathways. -
EGFR Inhibitor
Rociletinib hydrobromide is a selective inhibitor of mutant forms of the epidermal growth factor receptor (EGFR), particularly effective against the T790M mutation. It demonstrates a Ki value of 21.5 nM for the EGFRL858R/T790M variant, while maintaining a Ki of 303.3 nM for wild-type EGFR. This compound is relevant for research applications aimed at understanding and developing targeted therapies for EGFR-mutant cancers. -
EGFR Inhibitor
Tyrphostin AG 112 is a selective inhibitor of epidermal growth factor receptor (EGFR) phosphorylation. This compound has been shown to interfere with EGFR signaling pathways, resulting in the inhibition of cell proliferation and survival in various cancer cell lines. Tyrphostin AG 112 is utilized in research applications aimed at understanding EGFR-mediated processes and developing targeted therapies for EGFR-associated tumors. -
HER2/EGFR Inhibitor
Neratinib maleate is an orally available, irreversible inhibitor targeting HER2 and EGFR with IC50 values of 59 nM and 92 nM, respectively. This compound demonstrates significant anti-tumor activity and is utilized in research for its applications in cancer therapy, particularly in tumors exhibiting overexpression of HER2. Its selective inhibition profile makes it a valuable tool for studies exploring resistance mechanisms and therapeutic efficacy in targeted cancer treatment. -
EGFR-HER2 Inhibitor
Sevabertinib is a potent and reversible dual inhibitor of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2), exhibiting IC50 values below 0.5 nM for both wild-type HER2 and various mutant forms, including HER2 A775insYVMA, as well as wild-type EGFR and EGFR D770_N771insSVD. This compound demonstrates significant anticancer activity, particularly against lung cancer, making it a valuable tool for research in targeted cancer therapies and signaling pathway studies. -
EGFR/ErbB2 Inhibitor
PD 174265 is a highly selective, reversible inhibitor of the EGFR and ErbB2 tyrosine kinases, demonstrating an IC50 of 0.45 nM. This compound effectively inhibits receptor autophosphorylation and the downstream ERK signaling pathway, leading to significant antitumor activity and reduced toxicity in in vivo models. Additionally, PD 174265 facilitates the differentiation of oligodendrocyte precursor cells, promoting the expression of myelin proteins such as CNP, PLP, and MBP, and enhancing neurite branching. With no inhibitory effect on other kinases like insulin and PDGF receptors, PD 174265 is a vital tool for researching human epidermoid carcinoma treatment and myelin repair mechanisms in multiple sclerosis. -
EGFR/ERBB2 Inhibitor
HKI-357 is an irreversible dual inhibitor targeting EGFR and ERBB2, exhibiting IC50 values of 34 nM for EGFR and 33 nM for ERBB2. This compound effectively suppresses EGFR autophosphorylation at tyrosine 1068, leading to the inhibition of downstream signaling pathways, including AKT and MAPK phosphorylation. HKI-357 is valuable for research into cancer therapies that target these critical signaling pathways. -
EGFR Agonist
CN009543V is an agonist of the epidermal growth factor receptor (EGFR) that promotes tyrosine phosphorylation at residues Tyr1068 and Tyr1173, leading to the activation of the MAPK/ERK signaling cascade. Additionally, CN009543V inhibits protein tyrosine phosphatase 1B (PTP-1B) activity in MDA MB468 cancer cells. This compound is applicable in cancer research, particularly in studies focusing on EGFR signaling pathways and their implications in tumor biology. -
EGFR Inhibitor
EGFR-IN-70 is a potent inhibitor of the epidermal growth factor receptor (EGFR), exhibiting IC50 values of 23.6 nM and 307.5 nM for EGFR-LR/TM/CS and EGFR-WT, respectively. This compound demonstrates significant anti-proliferative effects and effectively suppresses EGFR phosphorylation. EGFR-IN-70 is a valuable tool for cancer research, particularly in studies focusing on EGFR-related signaling pathways and therapeutic interventions. -
EGFR Kinase Inhibitor
PF-06672131 is a potent inhibitor of the epidermal growth factor receptor (EGFR) kinase, targeting the ATP-binding pocket through its alkynylated afatinib derivative structure. This small molecule probe displays reactivity to cysteine and is valuable for activity-based protein profiling studies. Its ability to effectively inhibit EGFR makes it a useful tool in cancer research, particularly in exploring therapeutic strategies for EGFR-driven malignancies. -
EGFR Tyrosine Kinase Inhibitor
Mavelertinib is a highly selective, orally bioavailable irreversible inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. It demonstrates potent inhibitory activity with IC50 values of 5 nM, 4 nM, 12 nM, and 3 nM against Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. This compound is primarily utilized in research related to non-small-cell lung cancer (NSCLC). -
EGFR Inhibitor
Oritinib is an irreversible third-generation inhibitor targeting the epidermal growth factor receptor (EGFR). It effectively overcomes T790M-mediated resistance in non-small cell lung cancer by selectively inhibiting various mutant forms of EGFR, including EGFRWT, EGFRL858R, EGFRL861Q, and both EGFRL858R/T790M and EGFRd746-750 mutations, with low IC50 values ranging from 0.1 to 18 nM. This compound is valuable for research applications focusing on cancer therapeutics and mechanisms of drug resistance. -
Anti-EGFR/TGFβ Antibody
Ficerafusp alfa is a bispecific antibody targeting EGFR and TGFβ with a Kd of 2.58 nM for EGFR and 61.3 nM for TGFβ1. This compound inhibits EGFR phosphorylation, thereby blocking EGF-dependent cell proliferation and facilitating antibody-dependent cellular cytotoxicity in EGFR-positive tumor cells. Additionally, Ficerafusp alfa sequesters TGFβ via its TGFβRII ECD domain, neutralizing TGFβ activity and inhibiting TGFβ-dependent processes such as epithelial-mesenchymal transition. This reagent is valuable for research on head and neck squamous cell carcinoma, advanced solid tumors, and various cancers including squamous non-small cell lung cancer, anal squamous cell carcinoma, colorectal cancer, and pancreatic cancer. -
EGFR Inhibitor
EGFR-IN-95 is a potent inhibitor of the epidermal growth factor receptor (EGFR), specifically targeting del19/T790M/C797S and L858R/T790M/C797S mutations. This 2,4-diaminonicotinamide derivative exhibits strong biological activity, making it valuable for research on various EGFR-driven malignancies. Its use is particularly relevant in studies focused on developing targeted therapies for resistant forms of lung cancer and other EGFR-related conditions. -
Mutant-Selective EGFR Inhibitor
Osimertinib-d6 is a deuterium-labeled derivative of osimertinib, a covalent and orally active inhibitor that selectively targets mutant epidermal growth factor receptor (EGFR) variants. With an IC50 of 12 nM against the L858R mutation and 1 nM against L858R/T790M, osimertinib-d6 demonstrates potent efficacy in overcoming T790M-mediated resistance. This compound is valuable for research applications focused on targeted lung cancer therapies and the mechanisms of drug resistance in EGFR-driven tumors. -
EGFR Inhibitor
JCN037 is a non-covalent inhibitor targeting the epidermal growth factor receptor (EGFR) tyrosine kinase. It demonstrates potent activity with IC50 values of 2.49 nM for EGFR, 3.95 nM for p-wtEGFR, and 4.48 nM for pEGFRvIII, indicating its effectiveness in inhibiting various EGFR forms. This compound is particularly useful for research applications in cancer biology, especially in studies focused on EGFR signaling pathways and therapeutic resistance mechanisms. Its ability to penetrate the blood-brain barrier further extends its potential in neuro-oncological research. -
EGFR Inhibitor
(E/Z)-AG490 is a racemic mixture of the (E)-AG490 and (Z)-AG490 isomers, functioning as a potent inhibitor of the epidermal growth factor receptor (EGFR). This compound demonstrates inhibitory activity against other targets, including Stat-3 and the Janus kinases JAK2/3, making it valuable for research in signal transduction and cancer biology. Its ability to modulate key pathways involved in cell proliferation and survival positions (E/Z)-AG490 as an important tool for studying therapeutic strategies in oncology. -
EGFR Inhibitor
EGFR kinase inhibitor 3 is a bivalent ATP-allosteric inhibitor targeting the epidermal growth factor receptor (EGFR) kinase. It demonstrates potent inhibitory activity, with IC50 values of less than 10 nM for wild-type EGFR and as low as 0.059 nM for the L858R/T790M/C797S triple mutant. This compound is particularly useful for studies involving EGFR-mediated signaling pathways and can aid in the development of targeted therapies for EGFR-driven cancers. -
Alflutinib Metabolite/EGFR Inhibitor
AST5902 trimesylate is the primary metabolite of Alflutinib, functioning as an EGFR inhibitor. This compound demonstrates significant antineoplastic activity, making it a valuable reagent for cancer research. Its utility in exploring EGFR-related signaling pathways and therapeutic mechanisms can aid in the development of targeted cancer treatments. -
PROTAC EGFR Degrader
PROTAC EGFR Degrader 8 (T-184) is a proteolysis-targeting chimera (PROTAC) that specifically degrades the epidermal growth factor receptor (EGFR). With a DC50 of 15.56 nM in HCC827 cells, it effectively reduces EGFR levels and demonstrates potent growth inhibition in H1975, PC-9, and HCC827 cell lines, exhibiting IC50 values of 7.72 nM, 121.9 nM, and 14.21 nM, respectively. This compound is valuable for research focusing on cancer biology, particularly non-small cell lung cancer (NSCLC). -
EGFR Activator
13(S)-HPODE is a linoleic acid metabolite that acts as an EGFR activator. It has demonstrated significant biological activity in promoting cell proliferation and may play a role in various signaling pathways associated with cancer progression and inflammation. This compound is valuable for research into mechanisms of cancer biology and the development of therapeutic strategies targeting the EGFR pathway. -
EGFR-TKI Inhibitor
PKI-166 is a selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, demonstrating potent activity with an IC50 of 0.7 nM. It exhibits oral bioavailability and is utilized in research focused on cancer therapies that target aberrant EGFR signaling pathways. PKI-166 serves as a valuable tool for investigating the role of EGFR in tumorigenesis and evaluating the efficacy of EGFR-targeted treatments in various cancer models. -
EGFR/ErbB2 Inhibitor
Selatinib is a reversible and orally bioavailable dual inhibitor of epidermal growth factor receptor (EGFR) and ErbB2, demonstrating IC50 values of 13 nM and 22.5 nM, respectively. This compound exhibits significant anticancer activity, making it a valuable tool for research in targeted cancer therapies and studies focused on EGFR and ErbB2 signaling pathways. -
PROTAC EGFR Degrader
PROTAC EGFR Degrader 2 is a highly effective small molecule that targets the epidermal growth factor receptor (EGFR) for degradation via the PROTAC mechanism. It demonstrates significant antiproliferative activity with an IC50 of 4.0 nM, along with robust EGFR degradation activity, exhibiting a DC50 of 36.51 nM. This compound is suitable for applications in cancer research, particularly in exploring EGFR-related pathways and developing nitroreductase (NTR)-responsive PROTAC systems. -
EGFR Mutants Inhibitor
Pruvonertinib is an orally active inhibitor specifically targeting mutant forms of the epidermal growth factor receptor (EGFR), including the T790M mutation and exon 20 insertions. This compound has demonstrated significant antitumor activity, leading to tumor regression in patient-derived xenograft models driven by EGFR exon 20 insertions. Pruvonertinib is a valuable reagent for research in cancer biology, particularly in studies focused on resistant mutations in lung cancer therapeutics. -
EGFR Inhibitor
Simotinib is a selective, orally bioavailable inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, with an IC50 value of 19.9 nM. This compound exhibits significant antineoplastic activity, making it a valuable tool for cancer research. Simotinib is primarily utilized in studies investigating the molecular mechanisms of EGFR signaling and the development of targeted therapies for EGFR-dependent tumors. -
PROTAC EGFR Degrader
PROTAC EGFR Degrader 4 is a highly selective PROTAC designed to target mutant epidermal growth factor receptor (EGFR) variants. It effectively induces the degradation of EGFR del19 and the EGFR L858R/T790M double mutant, with DC50 values of 0.51 nM and 126 nM, respectively. This compound demonstrates significant growth inhibition in HCC827 and H1975 cell lines, exhibiting IC50 values of 0.83 nM and 203.1 nM. The degradation of EGFR is associated with autophagy, highlighting its potential in cancer research and therapeutic applications. -
EGFR
EGFR Protein Tyrosine Kinase Substrate serves as a substrate for the Epidermal Growth Factor Receptor (EGFR), facilitating the study of EGFR-mediated signaling pathways. This substrate is essential for investigating the catalytic activity of EGFR and its role in cellular processes such as proliferation and differentiation. It is particularly useful in research applications focusing on cancer biology, targeted therapies, and the development of EGFR inhibitors. -
EGFR Targeting Peptide
Cys-GE11 is a cysteine-modified peptide that targets the epidermal growth factor receptor (EGFR). This peptide can be conjugated via its thiol group, enabling the formation of targeted polymeric constructs to improve drug delivery efficacy. Cys-GE11 demonstrates enhanced enrichment of therapeutic agents at tumor sites, particularly in EGFR-overexpressing cells, such as SMMC-7721. Its utilization in research highlights its potential for applications in targeted cancer therapy with minimal toxicity. -
EGFR Inhibitor
BBT-176 is a potent oral inhibitor of the epidermal growth factor receptor (EGFR). It demonstrates significant inhibitory activity against various EGFR C797S mutant cell lines, making it a valuable tool for investigating resistance mechanisms in cancer therapy. This compound is widely utilized in cancer research to explore alternative treatment strategies targeting EGFR-related pathways. -
EGFR Inhibitor
EGFR-IN-197 is a potent inhibitor of the Epidermal Growth Factor Receptor (EGFR), displaying IC50 values of 19.5 nM and 12.0 nM against the EGFRL858R/T790M and EGFRL858R/T790M/C797S mutations, respectively. This compound effectively arrests the cell cycle in the G2/M phase, inhibiting proliferation, colony formation, and migration of NCI-H1975 cells. Additionally, EGFR-IN-197 disrupts anti-apoptotic signaling pathways, induces DNA damage, and activates pro-apoptotic pathways, thereby triggering apoptosis. Its properties make it a valuable reagent for research focused on non-small cell lung cancer (NSCLC). -
TrxR/EGFR Inhibitor
TrxR/EGFR-IN-1 is a potent inhibitor targeting both Thioredoxin Reductase (TrxR) and Epidermal Growth Factor Receptor (EGFR). This compound demonstrates significant anti-proliferative effects against Gefitinib-sensitive and resistant lung cancer cells, facilitating apoptosis and tumor cell death. TrxR/EGFR-IN-1 promotes GPX4 protein degradation via autophagolysosomal and proteasomal pathways, leading to ferroptosis. Additionally, it induces endoplasmic reticulum stress and triggers immunogenic cell death, making it a valuable tool for studying mechanisms underlying Gefitinib-resistant lung cancer. -
ErbB-2/EGFR Inhibitor
Lapatinib tosylate is a potent inhibitor targeting the ErbB-2 and EGFR tyrosine kinase domains. With IC50 values of 10.2 nM for EGFR and 9.8 nM for ErbB-2, it effectively blocks signaling pathways associated with cell proliferation and survival. This compound is primarily utilized in cancer research and therapeutic studies, particularly for conditions driven by aberrant ErbB signaling. -
EGFR Inhibitor
Afatinib N-Oxide is an oxidative degradation product of Afatinib dimaleate, an irreversible inhibitor of the epidermal growth factor receptor (EGFR) family. This compound serves as a valuable tool for characterizing the stability and degradation pathways of Afatinib in chemical research. It may also aid in understanding the mechanistic effects of EGFR inhibition in various biological contexts. -
AKT1/SRC/STAT3/EGFR Binder
(+)−Theta-cypermethrin is a stereoisomer of cypermethrin that functions as a selective binder to AKT1, SRC, STAT3, and epidermal growth factor receptor (EGFR). This compound is known to penetrate the blood-brain barrier, leading to alterations in the amplitude of delayed rectifier potassium channel currents and significant shifts in the activation and inactivation curves at elevated concentrations. Additionally, (+)-Theta-cypermethrin induces abnormal electrical activity in rat hippocampal neurons and is associated with chronic respiratory system damage and neurotoxicity. It serves as a valuable tool for research into signal transduction pathways and neuropharmacology. -
EGFR Ligand
Cyclo[K(N3)larllt] is a cyclic peptide that specifically targets the epidermal growth factor receptor (EGFR) with a Kd value of 5.09 μM and demonstrates selectivity for related proteins HER2 and HER3. This compound exhibits no cytotoxicity and does not inhibit the growth of EGFR-overexpressing cancer cells. Cyclo[K(N3)larllt] is ideal for use as a ligand in EGFR-targeted fluorescent conjugates, facilitating the detection of tumors with elevated EGFR levels. Its applications extend to research focused on colorectal cancer and related pathologies. -
EGFR Inhibitor
ZW-49 is a potent orally active pan-EGFR inhibitor, demonstrating IC50 values ranging from 0.03 to 1.5 nM. This compound selectively targets various EGFR mutations while sparing wild-type EGFR and other familial targets, effectively blocking the ATP-binding pocket and a conserved hydrophobic subpocket without causing steric conflicts with PACC mutation P loops. ZW-49 exhibits significant anti-proliferative activity by inhibiting cancer cell proliferation, inducing G0/G1 phase cell-cycle arrest, and promoting apoptosis, making it a valuable reagent for cancer research, particularly in non-small cell lung cancer models. -
EGFR Inhibitor
Rinumafusp alfa is a human monoclonal antibody that specifically inhibits the epidermal growth factor receptor (EGFR) by targeting ERBB3/HER3. This compound demonstrates potential in blocking tumor cell signaling pathways, thereby impeding tumor growth and progression. It is primarily utilized in research applications focused on cancer biology and therapeutic development targeting EGFR-related pathways. -
HER2 Inhibitor
JBJ-08-178-01 is a selective tyrosine kinase inhibitor targeting mutant forms of the human epidermal growth factor receptor 2 (HER2). It demonstrates significant antitumor activity by reducing both the kinase activity and protein levels of HER2 through the induction of proteasomal degradation. This compound holds potential for research applications in non-small-cell lung cancer, providing insights into therapeutic mechanisms against HER2-driven malignancies. -
EGFR PARP Dual-targeting PROTAC Molecule
DP-C-4 is a Cereblon-based dual-targeting PROTAC molecule designed for the concurrent degradation of epidermal growth factor receptor (EGFR) and poly (ADP-ribose) polymerase (PARP). This compound demonstrates significant biological activity by promoting the targeted destruction of these proteins, which can be crucial in cancer research and therapeutic applications. DP-C-4 may facilitate studies investigating the interplay between EGFR and PARP pathways, potentially leading to new insights in oncology and the development of innovative treatment strategies. -
ErbB-2/EGFR Tyrosine Kinase Inhibitor
GW583340 is an orally bioavailable inhibitor targeting the ErbB-2 and EGFR tyrosine kinases. It demonstrates significant antitumor activity in xenograft models characterized by overexpression of EGFR or ErbB-2, making it a valuable tool for investigating therapeutic strategies. GW583340 is particularly relevant for research focused on head and neck cancer, breast cancer, and gastric cancer. -
EGFR T790M/L858R/ACK1 Inhibitor
EGFR/ACK1-IN-1 is a potent inhibitor targeting the EGFR T790M/L858R mutation and ACK1, with IC50 values of 23 nM and 263 nM, respectively. This dual inhibition effectively disrupts cell proliferation and demonstrates significant antitumor activity. It is a valuable reagent for research applications focused on cancer biology and therapeutic development for EGFR mutant-driven tumors. -
EphB4, VEGFR-2 and PDGFR-β Inhibitor
JI-101 hydrochloride is an orally active inhibitor targeting EphB4, VEGFR-2, and PDGFR-β, effectively modulating angiogenesis signaling pathways associated with tumor vasculature. This compound demonstrates significant anti-cancer activity, inhibiting multiple stages of tumor angiogenesis and showing efficacy against various cancer cell lines and xenografts. With rapid oral absorption and extensive tissue distribution, preferential uptake occurs in the lungs, while elimination primarily occurs via feces. JI-101 hydrochloride can be utilized in research studies focused on ovarian cancer and other solid tumors, providing valuable insights into angiogenesis and cancer treatment mechanisms.
