EGFR/HER2

Cat. No.

A28738

CAS No.

2459932-81-9

EGFR-IN-49

EGFR-IN-49 is a selective inhibitor of the epidermal growth factor receptor (EGFR), exhibiting IC50 values of 65.0 nM for EGFRT790M and 13.6 nM for EGFRT790M/L858R variants. This compound effectively induces late apoptosis in a dose-dependent manner, making it a valuable tool for studying cancer cell signaling and apoptosis mechanisms. Its potency and selectivity position EGFR-IN-49 as a promising reagent for research applications focused on targeting EGFR-related pathways in cancer therapeutics.

Cat. No.

A28739

CAS No.

2758436-98-3

EGFR-IN-112

EGFR-IN-112 is a potent inhibitor of the EGFR kinase, exhibiting IC50 values of 2.31 ± 0.3 μM in MCF-7, 3.16 ± 0.8 μM in H69AR, and 4.2 ± 0.2 μM in PC-3 cancer cell lines. This compound shows selective cytotoxicity towards cancer cells, making it a valuable tool for research in targeted cancer therapies and investigations into EGFR-related signaling pathways. Its efficacy highlights its potential in the study of cancer resistance mechanisms and the development of novel anticancer treatments.

Cat. No.

A28740

CAS No.

1429497-30-2

BIEGi-1

BIEGi-1 is a selective inhibitor of the epidermal growth factor receptor (EGFR), primarily targeting the inhibition of EGFR-Rheb interactions within cells. It significantly suppresses EGFR kinase activity, as evidenced by reduced levels of p-Y1068-EGFR, and also impedes mTORC1 activation by lowering p-T389-S6K1 levels in EGFR-mutant cell lines. BIEGi-1 demonstrates pronounced antiproliferative effects on EGFR-mutant PC9 and HCC827 cells, exhibiting IC50 values of 17 nM and 20 nM, respectively. This compound is a valuable tool for investigating cancers associated with EGFR mutations, notably non-small cell lung cancer (NSCLC).

Cat. No.

A28742

CAS No.

1639040-91-7

EGFR-IN-199

EGFR-IN-199 is a potent and selective inhibitor of the epidermal growth factor receptor (EGFR), demonstrating IC50 values of 1.1 nM and 1.4 nM for purified EGFR wild-type and EGFRT790M/L858R kinases, respectively. This compound is valuable for cancer research, particularly in studies focused on EGFR signaling pathways and resistance mechanisms in tumor biology.

Cat. No.

A28743

CAS No.

2857033-34-0

EGFR-IN-73

EGFR-IN-73 is a selective inhibitor targeting the EGFR Del19 mutation, demonstrating an IC50 value of 119 nM. This compound exhibits potent inhibition of tumor proliferation driven by the prevalent EGFR Del19 mutation. It is suitable for research applications focusing on cancer biology and therapeutic development for EGFR-driven malignancies.

Cat. No.

A28745

CAS No.

2737283-20-2

EGFR ligand-2

EGFR ligand-2 (compound C4) is a covalent inhibitor targeting the epidermal growth factor receptor (EGFR), exhibiting IC50 values of 21 nM for the EGFRL858R mutant and 48 nM for the EGFRL858R/T790M double mutant. This compound is useful in studying EGFR mutations associated with various cancers and can be utilized in the synthesis of PROTACs for targeted protein degradation research applications.

Cat. No.

A28746

CAS No.

3031413-24-5

IAM1363

IAM1363 is a selective, irreversible inhibitor targeting the human epidermal growth factor receptor 2 (HER2). It demonstrates greater than 1,000-fold selectivity for HER2 over the epidermal growth factor receptor (EGFR), making it a valuable tool for investigating advanced HER2-positive cancers. This compound is particularly relevant for research on HER2-driven non-small cell lung cancer (NSCLC), facilitating the exploration of novel therapeutic strategies.

Cat. No.

A28748

CAS No.

2226257-92-5

NS-062

NS-062 is an orally active, irreversible inhibitor of the epidermal growth factor receptor (EGFR). It demonstrates significant antiproliferative activity in drug-resistant double mutated H1975 cells, with an IC50 value of 0.19 μM. Furthermore, NS-062 shows antitumor efficacy in an H1975 mouse xenograft model, making it a valuable tool for research on EGFR-related cancer treatments.

Cat. No.

A28749

CAS No.

847949-51-3

Gefitinib N-oxide

Gefitinib N-oxide is an N-oxide derivative of Gefitinib, acting as an inhibitor of the epidermal growth factor receptor (EGFR). It demonstrates a potent inhibitory effect, with an IC50 range of 2-37 nM in NR6wtEGFR cells. This compound is primarily utilized in research to investigate the modulation of EGFR signaling pathways and its implications in various cancer models.

Cat. No.

A28750

CAS No.

2711105-57-4

EGFR-IN-35

EGFR-IN-35 is a selective inhibitor of the epidermal growth factor receptor (EGFR), known for its role in regulating cell growth. This acrylamide derivative exhibits potent anti-tumor activity while maintaining a favorable safety profile. It is particularly relevant for studying cancers characterized by EGFR overexpression or mutations, such as non-small cell lung cancer (NSCLC). EGFR-IN-35 serves as a valuable tool for research into targeted therapies and mechanisms underlying EGFR-related oncogenesis.

Cat. No.

A28751

CAS No.

2648206-31-7

EGFR-IN-21

EGFR-IN-21 is a potent inhibitor of the epidermal growth factor receptor (EGFR), exhibiting an IC50 of 0.38 nM. This compound demonstrates significant antitumor activity, making it a valuable tool for research in cancer biology and therapeutic development. Its efficacy in inhibiting EGFR signals positions it for applications in studies focused on oncogenic pathways and targeted cancer treatments.

Cat. No.

A28752

CAS No.

2754392-31-7

EGFR-IN-28

EGFR-IN-28 is a potent inhibitor of the epidermal growth factor receptor (EGFR). This compound exhibits significant antitumor activity, making it a valuable tool in cancer research. EGFR-IN-28 is primarily utilized to study the mechanisms of tumor growth and response to targeted therapies in various malignancies.

Cat. No.

A28754

CAS No.

2841405-96-5

EGFR/CDK2-IN-1

EGFR/CDK2-IN-1 is an inhibitor targeting both the epidermal growth factor receptor (EGFR) and cyclin-dependent kinase 2 (CDK2). This compound exhibits significant cytotoxicity against breast cancer MCF7 cells and liver cancer HepG2 cells, making it a valuable tool in cancer research. Its dual inhibition profile allows for exploration of synergistic effects in therapeutic strategies targeting these critical pathways in cancer proliferation and survival.

Cat. No.

A28755

CAS No.

2906174-89-6

EGFR/BRAF-IN-1

EGFR/BRAF-IN-1 is a selective inhibitor targeting both EGFR and BRAFV600E with an IC50 of 45 nM. This compound, a 2,3-dihydropyrazino[1,2-a]indole-1,4-dione derivative, effectively inhibits cancer cell proliferation with a GI50 of 35 nM. Additionally, EGFR/BRAF-IN-1 exhibits notable antioxidant properties, making it a valuable reagent for research in cancer biology and therapeutic development.

Cat. No.

A28756

CAS No.

1781932-33-9

BMS-599626 dihydrochloride

BMS-599626 dihydrochloride is a small molecule pan-HER inhibitor that targets the human epidermal growth factor receptor family, specifically inhibiting HER1 (IC50=20 nmol/L) and HER2 (IC50=30 nmol/L) kinase activities. This compound functions by competing with ATP for binding to these receptors, thereby blocking their kinase activity and downstream signaling pathways through the inhibition of heterodimer formation between HER1 and HER2. BMS-599626 dihydrochloride serves as a valuable tool for investigating the antitumor effects in various tumor models overexpressing HER1 and HER2.

Cat. No.

A28757

CAS No.

1574321-31-5

EGFR-IN-139

EGFR-IN-139 is a potent inhibitor of the epidermal growth factor receptor (EGFR) with IC50 values of 12.88 nM for wild type, 10.84 nM for L858R/T790M, and 42.68 nM for L858R/T790M/C797S mutants. This compound exhibits significant anticancer activity in A549 and H1975 cell lines, demonstrating strong selectivity for cancer cells that overexpress EGFR. EGFR-IN-139 is particularly relevant for research focused on nonsmall cell lung cancer (NSCLC).

Cat. No.

A28758

CAS No.

1879071-97-2

EGFR/HER2-IN-5

EGFR/HER2-IN-5 is an orally active irreversible dual inhibitor targeting the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2). It exhibits a potent inhibitory effect on EGFR with an IC50 value of 1.01 nM and effectively inhibits EGFR kinase activity associated with L858R and T790M mutations. This compound demonstrates significant antitumor efficacy in vivo, making it a valuable tool for lung cancer research and the development of targeted therapies in oncology.

Cat. No.

A28759

CAS No.

2140807-58-3

JBJ-07-149

JBJ-07-149 is a potent EGFR inhibitor targeting the L858R/T790M mutations, exhibiting an IC50 of 1.1 nM. This compound effectively inhibits the proliferation of Ba/F3 cells, showing IC50 values of 4.9 μM and 0.148 μM in the absence and presence of Cetuximab, respectively. JBJ-07-149 serves as a useful ligand for the synthesis of DDC-01-163, facilitating research on EGFR-related pathways and therapeutic interventions in cancer.

Cat. No.

A28762

CAS No.

2820126-51-8

HER2-IN-12

HER2-IN-12 is a potent HER2 inhibitor with an IC50 value of 121 nM. It selectively targets the HER2 receptor, making it a valuable tool in cancer research, particularly in the study and treatment of breast cancer. Its efficacy in inhibiting HER2 activity supports investigations into therapeutic strategies for HER2-positive malignancies.

Cat. No.

A28765

CAS No.

2230253-82-2

PKI-166 hydrochloride

PKI-166 hydrochloride is a selective and potent inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, exhibiting an IC50 value of 0.7 nM. This compound is primarily utilized in cancer research, particularly in studies focused on EGFR-driven tumors. Its effectiveness in inhibiting EGFR activity makes it a valuable tool for investigating targeted therapies and understanding signaling pathways in oncogenesis.

Cat. No.

A28767

CAS No.

1346176-20-2

EGFR/HER2-IN-11

EGFR/HER2-IN-11 is a potent dual inhibitor targeting the human epidermal growth factor receptors HER2 and EGFR, demonstrating IC50 values of 7.7 nM and 22 nM, respectively. This compound exhibits significant antitumor activity and effectively inhibits the proliferation of cancer cells, specifically showing a GI50 of 601 nM against the BT-474 cell line. EGFR/HER2-IN-11 is suitable for research applications focused on cancer biology and therapeutic development targeting these key oncogenes.

Cat. No.

A28768

CAS No.

173458-56-5

CGP-59326

Synonyms: TRX-13

CGP-59326 is a potent and selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, with an IC50 of 0.027 μM. This compound effectively disrupts the EGFR signaling pathway, exhibiting strong inhibition of EGFR-dependent tumor cells. CGP-59326 is valuable for research applications in cancer biology, particularly in studies investigating EGFR-related malignancies.

Cat. No.

A28770

CAS No.

2676155-98-7

EGFR-IN-71

EGFR-IN-71 is a potent inhibitor of the epidermal growth factor receptor (EGFR), exhibiting an IC50 value of 3.7 μM. This compound is particularly useful in research focused on chordoma, providing a tool for studying EGFR-related signaling pathways. Additionally, EGFR-IN-71 features an alkyne group that facilitates copper-catalyzed azide-alkyne cycloaddition (CuAAc), enabling diverse applications in chemical biology and bioconjugation studies.

Cat. No.

A28771

CAS No.

3065211-08-4

EGFR-IN-193

EGFR-IN-193 is an inhibitor of the Epidermal Growth Factor Receptor (EGFR), primarily utilized in the synthesis of PROTACs as target protein ligands. It serves as a crucial component in the development of novel protein degradation strategies, particularly exemplified by PROTAC EGFR degrader 17, facilitating studies in cancer biology and targeted therapy research. This compound enables the exploration of EGFR signaling pathways and their roles in oncogenesis and tumor progression.

Cat. No.

A28772

CAS No.

2378188-21-5

EGFR/C797S-IN-1

EGFR/C797S-IN-1 is a selective inhibitor targeting the EGFR-C797S variant, demonstrating an IC50 of 0.128 µM. This compound exhibits significant anti-proliferative and anti-tumor effects, making it a valuable tool for cancer research. Notably, EGFR/C797S-IN-1 inhibits the phosphorylation of EGFR in a dose-dependent manner, contributing to its potential in therapeutic applications against resistant tumor phenotypes.