EGFR/HER2

Cat. No.

A28875

CAS No.

2772613-37-1

MS9427

MS9427 is a selective PROTAC degrader targeting the epidermal growth factor receptor (EGFR), demonstrating Kd values of 7.1 nM and 4.3 nM for EGFR wild-type and L858R mutant forms, respectively. This compound effectively induces degradation of the mutant EGFR via both the ubiquitin/proteasome system and autophagy/lysosomal pathways, while sparing the wild-type receptor. MS9427 is a valuable tool for studying the proliferation inhibition of non-small cell lung cancer (NSCLC) cells and advancing anticancer research.

Cat. No.

A28876

CAS No.

2820336-67-0

JBJ-09-063

JBJ-09-063 is a mutant-selective allosteric inhibitor targeting the epidermal growth factor receptor (EGFR). It exhibits potent inhibitory activity with IC50 values of 0.147 nM for EGFR L858R, 0.063 nM for EGFR L858R/T790M, 0.083 nM for EGFR L858R/T790M/C797S, and 0.396 nM for EGFR L747S. JBJ-09-063 effectively attenuates phosphorylation of EGFR, Akt, and ERK1/2, demonstrating its utility in both TKI-sensitive and resistant models. This compound is particularly valuable for studying EGFR-mutant lung cancer and exploring therapeutic strategies for treatment-resistant variants.

Cat. No.

A28877

CAS No.

2375107-27-8

Mutated EGFR-IN-3

Mutated EGFR-IN-3 is a highly selective allosteric inhibitor targeting the mutant forms of epidermal growth factor receptor (EGFR), specifically EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S). It demonstrates potent ATP-competitive inhibition with IC50 values of 12 nM and 13 nM, respectively. This compound is valuable for research applications focused on understanding and treating cancers driven by these specific EGFR mutations.

Cat. No.

A28879

CAS No.

2252334-12-4

Epitinib succinate

Synonyms: HMPL-813 succinate

Epitinib succinate is a selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) that demonstrates effective oral bioavailability and optimized penetration into the central nervous system. This compound is primarily utilized in cancer research, offering insights into targeted therapies for EGFR-associated tumors. Additionally, Epitinib succinate features an alkyne moiety that enables its use in click chemistry, specifically in copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, facilitating advanced biochemical studies.

Cat. No.

A28881

CAS No.

2817679-31-3

EGFR-IN-17

EGFR-IN-17 is a potent and selective inhibitor of the epidermal growth factor receptor (EGFR), exhibiting an IC50 value of 0.0002 μM. It is specifically designed to address C797S-mediated resistance, making it a valuable tool for researchers investigating EGFR-related pathways in cancer. This compound is applicable for studies focusing on therapeutic strategies against resistant forms of malignancies driven by EGFR signaling.

Cat. No.

A28884

CAS No.

202272-68-2

GW2974

GW2974 is a potent dual inhibitor of the human epidermal growth factor receptor 2 (HER2) and epidermal growth factor receptor (EGFR), with IC50 values of 0.007 μM and 0.016 μM, respectively. It effectively inhibits the proliferation of tumor cells in vitro, making it a valuable tool in cancer research. GW2974 is particularly relevant for studies focused on glioblastoma multiforme (GBM) and related malignancies.

Cat. No.

A28886

CAS No.

2675490-97-6

MS154N

MS154N is a negative control for the selective degradation of target proteins via the PROTAC (proteolysis targeting chimera) approach. Comprising an EGFR ligand, an E3 ligase ligand, and a PROTAC linker, this compound serves as a crucial investigational tool for validating the specificity and efficacy of PROTAC-based assays. Its design facilitates research into targeted protein degradation mechanisms, providing a reliable reference for experimental protocols involving MS39.

Cat. No.

A28888

CAS No.

2992670-44-5

EGFR ligand-9

EGFR ligand-9 is a specific ligand for the epidermal growth factor receptor (EGFR). It is designed for use in the synthesis of PROTAC EGFR degrader 9, facilitating the targeted degradation of EGFR in research applications. This compound is valuable for studying EGFR signaling pathways and developing novel therapeutic strategies in cancer research.

Cat. No.

A28889

CAS No.

76-80-2

Tephrosin

Synonyms: Deguelinol I; Hydroxydeguelin

Tephrosin is a natural rotenoid that functions as an inhibitor of the epidermal growth factor receptor (EGFR) and ErbB2. It demonstrates significant antitumor activity by promoting the internalization and subsequent degradation of these receptors, thereby disrupting downstream signaling pathways involved in cellular proliferation and survival. This compound is useful in cancer research, particularly in studies focusing on targeted therapies for EGFR and ErbB2-overexpressing tumors.

Cat. No.

A28890

CAS No.

3008543-34-5

EGFR/AURKB-IN-1

EGFR/AURKB-IN-1 is a dual inhibitor targeting Epidermal Growth Factor Receptor (EGFR) and Aurora Kinase B (AURKB), effectively blocking their phosphorylation with IC50 values of 0.07 µM and 1.1 µM, respectively. This compound binds to the hydrophobic region I and αC-helix out pocket of EGFR, as well as the back pocket of AURKB, thereby inhibiting tumor cell growth, division, and metastasis. EGFR/AURKB-IN-1 is suitable for comprehensive cancer research applications aimed at elucidating mechanisms of tumor progression and therapy resistance.

Cat. No.

A28892

CAS No.

1035638-91-5

PF-6274484

PF-6274484 is a highly selective inhibitor of the epidermal growth factor receptor (EGFR), with inhibitory constants (Kis) of 0.14 nM for the EGFR-L858R/T790M mutant and 0.18 nM for wild-type EGFR. This compound effectively inhibits autophosphorylation of EGFR-L858R/T790M in H1975 cells and wild-type EGFR in A549 cells, demonstrating IC50 values of 6.6 nM and 5.8 nM, respectively. PF-6274484 is valuable for researching targeted therapies in EGFR-driven cancers and elucidating signaling pathways linked to tumor proliferation.

Cat. No.

A28895

CAS No.

2682003-36-5

BI-4142

BI-4142 is a potent and highly selective inhibitor of the human epidermal growth factor receptor 2 (HER2), exhibiting an IC50 of 5 nM. This compound is primarily utilized in cancer research, particularly for studies involving HER2-overexpressing tumors. Its oral bioavailability and specificity make it an essential tool for investigating HER2 signaling pathways and potential therapeutic applications in oncology.

Cat. No.

A28896

CAS No.

2403760-72-3

Dosimertinib-d5 mesylate

Synonyms: AZD-9291-d5 mesylate; Mereletinib-d5 mesylate

Dosimertinib-d5 mesylate is a potent, orally active inhibitor of the epidermal growth factor receptor (EGFR). It effectively reduces the levels of phosphorylated EGFR and ERK proteins, demonstrating significant antiproliferative and anti-tumor activities. This compound is particularly relevant for research applications focused on non-small cell lung cancer (NSCLC).

Cat. No.

A28897

CAS No.

892772-75-7

EAI001

EAI001 is a potent allosteric inhibitor of the mutant epidermal growth factor receptor (EGFR), specifically targeting the EGFRL858R/T790M variant with an IC50 of 24 nM. This compound demonstrates selective inhibition of aberrant EGFR signaling, making it valuable for investigating its role in cancer biology and therapeutic resistance. EAI001 serves as a critical tool for research aimed at understanding and developing treatments for EGFR-mutated tumors.

Cat. No.

A28898

CAS No.

179248-61-4

EGFR/ErbB-2-IN-2

EGFR/ErbB-2-IN-2 is a potent inhibitor of the epidermal growth factor receptor (EGFR) and ErbB family of receptor tyrosine kinases. It exhibits IC50 values of 0.017 μM for EGFR, 0.08 μM for ErbB-2, and 1.91 μM for ErbB-4, highlighting its selectivity and efficacy. This compound is valuable for research applications focused on cancer biology, particularly in the study of signaling pathways and mechanisms associated with EGFR and ErbB receptor activation.

Cat. No.

A28900

CAS No.

1622327-37-0

Laprituximab emtansine

Synonyms: IMGN-289; J2898A-SMCC-DM1

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.

Cat. No.

A28901

CAS No.

1446700-26-0

Rociletinib hydrobromide

Synonyms: CO-1686 hydrobromide; AVL-301 hydrobromide; CNX-419 hydrobromide

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.

Cat. No.

A28902

CAS No.

144978-82-5

Tyrphostin AG 112

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.

Cat. No.

A28906

CAS No.

915942-22-2

Neratinib maleate

Synonyms: HKI-272 maleate

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.

Cat. No.

A28907

CAS No.

2521285-05-0

Sevabertinib

Synonyms: BAY 2927088

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.

Cat. No.

A28908

CAS No.

216163-53-0

PD 174265

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.

Cat. No.

A28909

CAS No.

848133-17-5

HKI-357

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.

Cat. No.

A28917

CAS No.

375826-84-9

CN009543V

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.

Cat. No.

A28919

CAS No.

2926716-96-1

EGFR-IN-70

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.

Cat. No.

A28920

CAS No.

1621002-27-4

PF-06672131

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.