EGFR/HER2

Cat. No.

A28836

CAS No.

2711105-54-1

EGFR-IN-36

EGFR-IN-36 is a selective inhibitor of the epidermal growth factor receptor (EGFR), exhibiting IC50 values of 19.09 nM, 120.01 nM, and 2.35 nM for wild-type EGFR, wild-type HER2, and the HER2 mutant A775_G776insYVMA, respectively. This compound demonstrates significant potential in research focused on tumor types driven by both wild-type and mutant forms of EGFR and HER2 kinases, making it a valuable tool for investigating targeted cancer therapies.

Cat. No.

A28838

CAS No.

2749562-63-6

EGFR-IN-25

EGFR-IN-25 is a potent inhibitor of the epidermal growth factor receptor (EGFR) with IC50 values of 9 nM in BaF3 cells harboring the EGFR DEL19/T790M/C797S mutation and 60 nM in A431 cells expressing wild-type EGFR. This compound exhibits significant biological activity that supports its application in cancer research, particularly in studies targeting EGFR-driven tumors. EGFR-IN-25 can be utilized to investigate the effects of EGFR inhibition on cell proliferation and survival in relevant preclinical models.

Cat. No.

A28839

CAS No.

2170255-78-2

Rezivertinib hydrochloride

Synonyms: BPI-7711 hydrochloride

Rezivertinib hydrochloride is a highly selective and irreversible third-generation inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. It demonstrates potent activity against both the common EGFR activating mutations and the T790M resistance mutation. This compound also possesses excellent central nervous system (CNS) penetration, making it a valuable tool in the study of antitumor activity, particularly in the context of non-small cell lung cancer (NSCLC). Researchers may utilize Rezivertinib hydrochloride to investigate mechanisms of resistance and evaluate therapeutic strategies targeting EGFR-related pathways.

Cat. No.

A28840

CAS No.

2387570-03-6

(R)-DZD1516

(R)-DZD1516 is the R enantiomer of DZD1516, serving as a potent and selective inhibitor of the HER2 receptor. This compound demonstrates significant inhibition of HER2 signaling pathways, which are often implicated in the progression of various cancers. (R)-DZD1516 is valuable for research applications focused on cancer biology, particularly in studies evaluating therapeutic strategies targeting HER2-positive tumors.

Cat. No.

A28843

CAS No.

2500674-05-3

Pertuzumab zuvotolimod

Synonyms: SBT6050

Pertuzumab zuvotolimod is an anti-HER2 antibody-drug conjugate (ADC) designed to target HER2-positive tumors. The combination of a humanized anti-HER2 antibody, Pertuzumab, with a TLR8 agonist payload and a linker enhances anti-tumor immune responses by activating myeloid cells and inducing T and NK cell cytolytic activity. This reagent is suitable for research focused on HER2-expressing solid tumors, providing a valuable tool for studying therapeutic strategies in this area.

Cat. No.

A28844

CAS No.

2757548-54-0

EGFR-IN-24

EGFR-IN-24 is a selective inhibitor of the epidermal growth factor receptor (EGFR), demonstrated to effectively target both EGFR mutations del19/T790M/C797S and L858R/T790M/C797S. This compound exhibits significant antiproliferative activity, making it a valuable tool in cancer research, particularly for studies focused on non-small cell lung cancer and resistance mechanisms associated with EGFR mutations. Researchers can utilize EGFR-IN-24 to explore therapeutic strategies and develop potential treatment options for patients harboring these challenging mutations.

Cat. No.

A28845

CAS No.

122520-79-0

Tyrphostin AG30

Synonyms: AG30

Tyrphostin AG30 is a selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. It effectively inhibits self-renewal induction mediated by c-ErbB and obstructs the activation of STAT5 by c-ErbB in primary erythroblasts. This compound serves as a valuable tool in cancer research, particularly in studies focused on EGFR signaling pathways and their role in tumor proliferation and growth.

Cat. No.

A28846

CAS No.

944342-90-9

JNJ28871063 hydrochloride

JNJ28871063 hydrochloride is a highly selective and orally active pan-ErbB kinase inhibitor that targets ErbB1, ErbB2, and ErbB4 with IC50 values of 22 nM, 38 nM, and 21 nM, respectively. This compound effectively inhibits the phosphorylation of critical tyrosine residues in EGFR and ErbB2, disrupting signaling pathways implicated in tumorigenesis. Additionally, JNJ28871063 hydrochloride is capable of crossing the blood-brain barrier and has demonstrated significant antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2.

Cat. No.

A28847

CAS No.

35773-42-3

EMI1

EMI1 is a selective inhibitor of mutant epidermal growth factor receptor (EGFR) variants, specifically ex19del/T790M/C797S and L858R/T790M/C797S. This compound demonstrates significant efficacy against drug-resistant non-small-cell lung cancer (NSCLC) associated with these mutations. EMI1 serves as a valuable tool for research investigating the molecular mechanisms of EGFR-related resistance and potential therapeutic strategies in NSCLC.

Cat. No.

A28851

CAS No.

1402086-20-7

Afatinib impurity 11

Afatinib impurity 11 is an impurity associated with Afatinib, a well-known irreversible inhibitor of the epidermal growth factor receptor (EGFR) family. Afatinib exhibits potent biological activity, with IC50 values of 0.5 nM, 0.4 nM, 10 nM, and 14 nM against wild-type EGFR, EGFRL858R, EGFRL858R/T790M, and HER2, respectively. This compound is essential for investigating the purity and synthesis of Afatinib, contributing to research focused on targeted cancer therapies.

Cat. No.

A28852

CAS No.

2414056-31-6

Perzebertinib

Synonyms: ZN-A-1041

Perzebertinib is a potent HER2 inhibitor that demonstrates significant activity in inhibiting BT474 cells with an IC50 of 9.5 nM. Additionally, it targets wild-type EGFR in H838 cells, exhibiting an IC50 of 12 µM. This compound is applicable for research into pathways associated with cancer and inflammation.

Cat. No.

A28853

CAS No.

1203902-67-3

Epitinib

Synonyms: HMPL-813

Epitinib is an orally active and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI), designed to achieve optimal penetration into the brain. This compound is particularly useful in cancer research due to its ability to inhibit EGFR signaling pathways. Additionally, Epitinib contains an alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions, which can be harnessed in click chemistry applications for various biological studies.

Cat. No.

A28855

CAS No.

2681392-19-6

BI-1622

BI-1622 is a potent and highly selective inhibitor of HER2 (ERBB2), exhibiting an IC50 of 7 nM. This compound demonstrates over 25-fold selectivity against EGFR, making it a valuable tool in targeted cancer therapy. In vivo studies using xenograft mouse models with engineered H2170 and PC9 cells reveal significant antitumor efficacy. Additionally, BI-1622 possesses favorable pharmacokinetic and metabolic properties, supporting its potential for clinical research applications.

Cat. No.

A28856

CAS No.

2364326-23-6

SPH5030

SPH5030 is a selective and irreversible inhibitor of the HER2 receptor, targeting both HER2WT and EGFRWT with IC50 values of 3.51 nM and 8.13 nM, respectively. This compound demonstrates significant activity against various HER2 mutant forms, making it a valuable tool in cancer research. SPH5030 is useful for studying HER2-related pathways and developing targeted therapies for HER2-positive cancers.

Cat. No.

A28857

CAS No.

1034651-23-4

Erlotinib-d6

Synonyms: CP-358774-d6; NSC 718781-d6; OSI-774-d6

Erlotinib-d6 is a deuterated analog of Erlotinib, specifically targeting the epidermal growth factor receptor (EGFR) as a tyrosine kinase inhibitor. With an IC50 of 2 nM for human EGFR, it demonstrates potent inhibitory activity crucial for studying EGFR-mediated signaling pathways. As a click chemistry reagent, Erlotinib-d6 contains an alkyne functional group, enabling copper-catalyzed azide-alkyne cycloaddition (CuAAc) for applications in chemical biology and bioconjugation research.

Cat. No.

A28859

CAS No.

1807453-44-6

EGFR-IN-122

EGFR-IN-122 is a potent inhibitor of the epidermal growth factor receptor (EGFR), a critical target in cancer therapy. This compound effectively suppresses the proliferation of EGFR-driven cancer cell lines, specifically PC-9GR and HCC827GR. Its use in research applications contributes to the understanding of EGFR signaling pathways and aids in the development of targeted therapies for EGFR-dependent tumors.

Cat. No.

A28863

CAS No.

2413029-40-8

EGFR-IN-89

EGFR-IN-89 is a potent fourth-generation inhibitor targeting the EGFR C797S mutation, demonstrating an IC50 of 10.1 nM against Del19/T790M/C797S mutations. This compound exhibits enhanced selectivity over wild-type EGFR, making it a valuable tool for studying resistance mechanisms in non-small cell lung cancer (NSCLC) and other malignancies with EGFR mutations. Its application can significantly aid in the development of targeted therapies for patients with specific EGFR mutations.

Cat. No.

A28864

CAS No.

2254145-43-0

Andamertinib

Andamertinib is a selective inhibitor of the epidermal growth factor receptor (EGFR), exhibiting significant antineoplastic activity. This compound is primarily utilized in research related to targeted cancer therapies, particularly in the treatment of EGFR-mutant cancers. Its mechanism of action involves blocking EGFR signaling pathways, thereby inhibiting tumor growth and proliferation.

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.