EGFR/HER2

Cat. No.

A28806

CAS No.

2433837-65-9

EGFR-IN-69

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.

Cat. No.

A28807

CAS No.

1173023-85-2

GW583340 dihydrochloride

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.

Cat. No.

A28808

CAS No.

2851060-90-5

HLX-22

Synonyms: AC101

HLX-22 is a humanized monoclonal antibody that specifically targets HER2, a receptor often overexpressed in certain cancer types. This antibody exhibits significant anti-tumor activity by inducing apoptosis in HER2-overexpressing breast and gastric cancer cells, particularly in combination with Trastuzumab. HLX-22 is primarily utilized in research focused on advanced solid tumors, making it a valuable tool in the study of targeted cancer therapies.

Cat. No.

A28810

CAS No.

1983-81-9

4,7-Dihydroxycoumarin

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.

Cat. No.

A28811

CAS No.

345615-74-9

Tyrosine kinase-IN-7

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.

Cat. No.

A28813

CAS No.

2140806-84-2

DDC-01-163

DDC-01-163 is an allosteric PROTAC degrader that targets the epidermal growth factor receptor (EGFR) through the ubiquitin-proteasome system. It demonstrates selective inhibition of L858R/T790M mutant Ba/F3 cell proliferation and is effective against resistant variants, including L/T/C797S and L/T/L718Q EGFR mutations. DDC-01-163 exhibits enhanced anti-proliferative effects in combination with the ATP-site EGFR inhibitor Osimertinib, making it a valuable tool for studying non-small cell lung cancer.

Cat. No.

A28815

CAS No.

2089721-94-6

ES-072

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.

Cat. No.

A28816

CAS No.

27257-15-4

1-Methyl-1H-pyrrolo[2,3-b]pyridine

1-Methyl-1H-pyrrolo[2,3-b]pyridine is an EGFR-binding agent that selectively inhibits the kinase domain of the epidermal growth factor receptor. This compound demonstrates efficacy in inhibiting the proliferation of breast cancer cells while exhibiting no significant activity against lung and liver cancer cells. It serves as a valuable tool in breast cancer research, providing insights into EGFR-mediated signaling pathways and potential therapeutic strategies.

Cat. No.

A28817

CAS No.

1644502-33-9

BPI-15086

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.

Cat. No.

A28818

CAS No.

1821329-75-2

Derazantinib dihydrochloride

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.

Cat. No.

A28819

CAS No.

2413487-72-4

Theliatinib tartrate

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.

Cat. No.

A28820

CAS No.

2403760-70-1

Dosimertinib-d3

Dosimertinib-d3 is a potent inhibitor of the epidermal growth factor receptor (EGFR). This compound effectively reduces levels of phosphorylated EGFR and ERK proteins, exhibiting significant antiproliferative and antitumor activities. Dosimertinib-d3 is particularly relevant for research applications targeting non-small-cell lung cancer (NSCLC) and offers a valuable tool for studying EGFR-mediated signaling pathways.

Cat. No.

A28821

CAS No.

2748162-29-8

JBJ-02-112-05

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.

Cat. No.

A28822

CAS No.

2389149-85-1

Mobocertinib mesylate

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).

Cat. No.

A28823

CAS No.

2820447-02-5

EGFR/CSC-IN-1

EGFR/CSC-IN-1 is a potent inhibitor of the epidermal growth factor receptor (EGFR) with an IC50 of 10.52 nM, and it also targets cancer stem cells (CSCs). This dual inhibition is particularly relevant for research focused on triple-negative breast cancer, offering a pathway to explore therapeutic strategies that may improve treatment outcomes in this aggressive malignancy.

Cat. No.

A28824

CAS No.

2701563-03-1

EGFR-IN-31

EGFR-IN-31 is a selective inhibitor of the epidermal growth factor receptor (EGFR), a key protein implicated in the regulation of cell proliferation and survival. The overexpression and mutation of EGFR are linked to various cancers, particularly non-small cell lung cancer (NSCLC). This compound is designed for research focused on the role of EGFR mutations in disease progression and may aid in the development of targeted therapies for EGFR-related malignancies.

Cat. No.

A28826

CAS No.

2180164-79-6

Oritinib mesylate

Synonyms: SH-1028 mesylate

Oritinib mesylate is a selective, orally active irreversible inhibitor of the epidermal growth factor receptor (EGFR) with an IC50 of 18 nM. This compound demonstrates strong activity against both EGFR-sensitive and T790M-resistant mutations. Oritinib mesylate effectively inhibits the proliferation of tumor cells harboring these mutations, making it a valuable tool for research in cancer biology and targeted therapies.

Cat. No.

A28827

CAS No.

2568506-66-9

EGFR-IN-103

EGFR-IN-103 is a highly potent inhibitor of the epidermal growth factor receptor (EGFR), exhibiting an IC50 value of 6 nM for phosphorylated EGFR (pEGFR). This compound demonstrates effective inhibition of EGFR-mediated signaling pathways, making it valuable in cancer research, particularly in drug resistance studies and therapeutic applications targeting EGFR-driven tumors. Its specificity and potency make it an essential tool for studying EGFR-related biological processes and evaluating new therapeutic strategies.

Cat. No.

A28828

CAS No.

2691891-38-8

HER2-IN-6

HER2-IN-6 is a potent inhibitor of the HER2 receptor, targeting its kinase activity. This compound demonstrates significant efficacy against both wild-type and mutant forms of HER2, making it valuable for research focused on HER2-mediated tumorigenesis. Additionally, HER2-IN-6 may serve as a useful tool in studies investigating the role of HER2 in various cancer types.

Cat. No.

A28829

CAS No.

34564-13-1

EMI48

EMI48 is a selective inhibitor targeting the EGFR triple mutant variant. It exhibits enhanced potency compared to its predecessor, EMI1, effectively inhibiting the activity of mutant EGFR. This compound is valuable for research focused on understanding the mechanisms of resistance in cancer therapy and evaluating therapeutic strategies against EGFR-mutant tumors.

Cat. No.

A28830

CAS No.

2850355-96-1

Vislarafusp alfa

Vislarafusp alfa is a humanized IgG1κ antibody targeting both EGFR and CD47. This novel bispecific antibody exhibits potential for modulating tumor immune evasion and promoting anti-tumor responses, making it significant in cancer research applications. Its unique mechanism of action presents valuable opportunities for studying combination therapies and understanding the interplay between immune checkpoint regulators and growth factor signaling pathways.

Cat. No.

A28831

CAS No.

2573869-16-4

EGFR-IN-15

EGFR-IN-15 is a potent inhibitor of the epidermal growth factor receptor (EGFR), exhibiting an IC50 of 4 nM. This compound is pivotal for research in oncological diseases, allowing for the exploration of EGFR signaling pathways and their role in tumorigenesis. Its high specificity and efficacy make it a valuable tool for therapeutic investigations and drug development targeting EGFR-driven malignancies.

Cat. No.

A28832

CAS No.

1215571-02-0

EGFR/HER2-IN-2

EGFR/HER2-IN-2 is a dual inhibitor targeting the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2). It demonstrates potent inhibitory activity with IC50 values of 5.02 µM for EGFR and 0.83 µM for HER2. This compound is valuable for research applications focusing on cancer biology, particularly in the study of EGFR and HER2 signaling pathways and their role in tumor proliferation and resistance mechanisms.

Cat. No.

A28834

CAS No.

2769714-36-3

BI-8128

BI-8128 is a potent inhibitor of the epidermal growth factor receptor (EGFR), exhibiting IC50 values of 12 nM for wild-type and 3 nM for the L858R/T790M/C797S mutant variants. This compound effectively inhibits the proliferation of Ba/F3 and PC-9 cells that are resistant to conventional therapies. BI-8128 is particularly relevant for research focused on non-small cell lung cancer, providing valuable insights into resistance mechanisms and potential therapeutic strategies.

Cat. No.

A28835

CAS No.

2691891-36-6

HER2-IN-5

HER2-IN-5 is a potent, orally active inhibitor of the HER2 receptor, targeting its role in the proliferation and survival of cancer cells. As a promising agent in cancer research, HER2-IN-5 demonstrates significant anticancer activity by disrupting HER2 signaling pathways. It has potential applications in the development of therapies for HER2-positive cancers, providing a valuable tool for investigating HER2-related mechanisms in oncology.