EGFR/HER2

Cat. No.

A28865

CAS No.

1858291-14-1

(3S,4S)-PF-06459988

(3S,4S)-PF-06459988 is a selective irreversible inhibitor targeting the T790M mutant form of the epidermal growth factor receptor (EGFR). This compound demonstrates significant biological activity against mutant EGFR while exhibiting excellent selectivity for the wild-type receptor. Its design features a minimally reactive electrophile, which reduces the likelihood of off-target labeling, making it a valuable reagent for cancer research and studies investigating EGFR-driven pathways.

Cat. No.

A28866

CAS No.

63177-57-1

Methyl 2,5-dihydroxycinnamate

Methyl 2,5-dihydroxycinnamate is a potent inhibitor of epidermal growth factor receptor (EGFR) kinase activity, functioning as an erbstatin analog. This compound effectively disrupts EGFR signaling, making it a valuable tool in cancer research, particularly for studies focused on tumor growth and metastasis. Its stability and efficacy position it as an important reagent for elucidating the role of EGFR in various biological processes.

Cat. No.

A28867

CAS No.

2050906-40-4

BEBT-109

BEBT-109 is a potent pan-mutant-selective inhibitor of the epidermal growth factor receptor (EGFR). This compound exhibits enhanced pharmacokinetic properties, making it suitable for in-depth studies. BEBT-109 is primarily utilized in research focused on non-small cell lung cancer (NSCLC) driven by various EGFR mutations, enabling exploration of therapeutic strategies targeting this pathway.

Cat. No.

A28871

CAS No.

2227455-78-7

EGFR-IN-1 hydrochloride

EGFR-IN-1 hydrochloride is an orally active and irreversible inhibitor targeting the mutant EGFR L858R/T790M. This compound exhibits potent inhibition of Gefitinib-resistant EGFR variants with a selectivity ratio of 100-fold over wild-type EGFR. Notably, EGFR-IN-1 hydrochloride demonstrates significant antiproliferative activity against H1975 and HCC827 cell lines, making it a valuable tool for antitumor research applications in cancer studies related to resistant EGFR mutations.

Cat. No.

A28872

CAS No.

2414374-41-5

EMI56

EMI56 is a potent inhibitor of the EGFR triple mutant, demonstrating enhanced activity compared to its precursor, EMI1. This compound effectively targets and inhibits mutant forms of the epidermal growth factor receptor, making it valuable for research into EGFR-related pathologies, particularly in cancer models. EMI56 is suitable for studies focused on understanding resistance mechanisms and developing targeted therapeutic strategies.

Cat. No.

A28873

CAS No.

2489185-38-6

Enozertinib

Synonyms: ORIC-114

Enozertinib is a potent dual inhibitor of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2), designed for oral administration with the ability to penetrate the central nervous system. This highly selective and irreversible compound effectively targets exon 20 insertion mutations, demonstrating significant antitumor activity and inducing tumor regression in models of central nervous system and non-small cell lung cancer (NSCLC). Enozertinib is valuable for research involving solid tumors and NSCLC, offering enhanced kinome selectivity to minimize off-target effects.

Cat. No.

A28874

CAS No.

1625677-63-5

EGFR-IN-1

EGFR-IN-1 is an orally active, irreversible inhibitor selectively targeting the EGFR L858R/T790M mutants. This compound demonstrates potent inhibition of Gefitinib-resistant EGFR variants with over 100-fold selectivity compared to wild-type EGFR. EGFR-IN-1 exhibits significant antiproliferative effects in both H1975 and mutated HCC827 cancer cell lines, indicating its potential utility in anticancer research and therapeutic applications.

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.

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.

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.

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.

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.