EGFR/HER2

Cat. No.

A28921

CAS No.

1776112-90-3

Mavelertinib

Synonyms: PF-06747775

Mavelertinib is a highly selective, orally bioavailable irreversible inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. It demonstrates potent inhibitory activity with IC50 values of 5 nM, 4 nM, 12 nM, and 3 nM against Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. This compound is primarily utilized in research related to non-small-cell lung cancer (NSCLC).

Cat. No.

A28923

CAS No.

2035089-28-0

Oritinib

Synonyms: SH-1028

Oritinib is an irreversible third-generation inhibitor targeting the epidermal growth factor receptor (EGFR). It effectively overcomes T790M-mediated resistance in non-small cell lung cancer by selectively inhibiting various mutant forms of EGFR, including EGFRWT, EGFRL858R, EGFRL861Q, and both EGFRL858R/T790M and EGFRd746-750 mutations, with low IC50 values ranging from 0.1 to 18 nM. This compound is valuable for research applications focusing on cancer therapeutics and mechanisms of drug resistance.

Cat. No.

A28924

CAS No.

881001-19-0

EGFR/ErbB-2/ErbB-4 inhibitor-3

EGFR/ErbB-2/ErbB-4 inhibitor-3 functions as a potent tyrosine kinase inhibitor, exhibiting IC50 values of 0.3 nM for ErbB1, 1.1 nM for ErbB2, and 0.5 nM for ErbB4. This compound serves as a valuable tool in cancer research, particularly in studies targeting EGFR-related signaling pathways. Additionally, it features an alkyne group, enabling its use in copper-catalyzed azide-alkyne cycloaddition (CuAAc), thus facilitating bioconjugation applications in chemical biology.

Cat. No.

A28928

CAS No.

2764727-44-6

Ficerafusp alfa

Synonyms: BCA-101; FMAB2

Ficerafusp alfa is a bispecific antibody targeting EGFR and TGFβ with a Kd of 2.58 nM for EGFR and 61.3 nM for TGFβ1. This compound inhibits EGFR phosphorylation, thereby blocking EGF-dependent cell proliferation and facilitating antibody-dependent cellular cytotoxicity in EGFR-positive tumor cells. Additionally, Ficerafusp alfa sequesters TGFβ via its TGFβRII ECD domain, neutralizing TGFβ activity and inhibiting TGFβ-dependent processes such as epithelial-mesenchymal transition. This reagent is valuable for research on head and neck squamous cell carcinoma, advanced solid tumors, and various cancers including squamous non-small cell lung cancer, anal squamous cell carcinoma, colorectal cancer, and pancreatic cancer.

Cat. No.

A28929

CAS No.

3027135-04-9

EGFR-IN-95

EGFR-IN-95 is a potent inhibitor of the epidermal growth factor receptor (EGFR), specifically targeting del19/T790M/C797S and L858R/T790M/C797S mutations. This 2,4-diaminonicotinamide derivative exhibits strong biological activity, making it valuable for research on various EGFR-driven malignancies. Its use is particularly relevant in studies focused on developing targeted therapies for resistant forms of lung cancer and other EGFR-related conditions.

Cat. No.

A28930

CAS No.

1638281-44-3

Osimertinib-d6

Synonyms: AZD-9291-d6; Mereletinib-d6

Osimertinib-d6 is a deuterium-labeled derivative of osimertinib, a covalent and orally active inhibitor that selectively targets mutant epidermal growth factor receptor (EGFR) variants. With an IC50 of 12 nM against the L858R mutation and 1 nM against L858R/T790M, osimertinib-d6 demonstrates potent efficacy in overcoming T790M-mediated resistance. This compound is valuable for research applications focused on targeted lung cancer therapies and the mechanisms of drug resistance in EGFR-driven tumors.

Cat. No.

A28931

CAS No.

2305154-31-6

JCN037

Synonyms: JGK037

JCN037 is a non-covalent inhibitor targeting the epidermal growth factor receptor (EGFR) tyrosine kinase. It demonstrates potent activity with IC50 values of 2.49 nM for EGFR, 3.95 nM for p-wtEGFR, and 4.48 nM for pEGFRvIII, indicating its effectiveness in inhibiting various EGFR forms. This compound is particularly useful for research applications in cancer biology, especially in studies focused on EGFR signaling pathways and therapeutic resistance mechanisms. Its ability to penetrate the blood-brain barrier further extends its potential in neuro-oncological research.

Cat. No.

A28933

CAS No.

134036-52-5

(E/Z)-AG490

Synonyms: (E/Z)-Tyrphostin AG490; (E/Z)-Tyrphostin B42

(E/Z)-AG490 is a racemic mixture of the (E)-AG490 and (Z)-AG490 isomers, functioning as a potent inhibitor of the epidermal growth factor receptor (EGFR). This compound demonstrates inhibitory activity against other targets, including Stat-3 and the Janus kinases JAK2/3, making it valuable for research in signal transduction and cancer biology. Its ability to modulate key pathways involved in cell proliferation and survival positions (E/Z)-AG490 as an important tool for studying therapeutic strategies in oncology.

Cat. No.

A28934

CAS No.

2922402-03-5

EGFR kinase inhibitor 3

EGFR kinase inhibitor 3 is a bivalent ATP-allosteric inhibitor targeting the epidermal growth factor receptor (EGFR) kinase. It demonstrates potent inhibitory activity, with IC50 values of less than 10 nM for wild-type EGFR and as low as 0.059 nM for the L858R/T790M/C797S triple mutant. This compound is particularly useful for studies involving EGFR-mediated signaling pathways and can aid in the development of targeted therapies for EGFR-driven cancers.

Cat. No.

A28935

CAS No.

2387570-00-3

DZD1516

DZD1516 is a highly potent and selective inhibitor of the HER2 receptor, exhibiting an IC50 value of 0.56 nM. This compound demonstrates significant antitumor activity in both central nervous system and subcutaneous xenograft mouse models, making it a valuable tool for research in cancer therapeutics targeting HER2-positive tumors. Its favorable blood-brain permeability further enhances its potential utility in investigating CNS-related malignancies.

Cat. No.

A28936

CAS No.

2929417-90-1

AST5902 trimesylate

AST5902 trimesylate is the primary metabolite of Alflutinib, functioning as an EGFR inhibitor. This compound demonstrates significant antineoplastic activity, making it a valuable reagent for cancer research. Its utility in exploring EGFR-related signaling pathways and therapeutic mechanisms can aid in the development of targeted cancer treatments.

Cat. No.

A28937

CAS No.

2925923-46-0

PROTAC EGFR degrader 8

PROTAC EGFR Degrader 8 (T-184) is a proteolysis-targeting chimera (PROTAC) that specifically degrades the epidermal growth factor receptor (EGFR). With a DC50 of 15.56 nM in HCC827 cells, it effectively reduces EGFR levels and demonstrates potent growth inhibition in H1975, PC-9, and HCC827 cell lines, exhibiting IC50 values of 7.72 nM, 121.9 nM, and 14.21 nM, respectively. This compound is valuable for research focusing on cancer biology, particularly non-small cell lung cancer (NSCLC).

Cat. No.

A28938

CAS No.

33964-75-9

13(S)-HPODE

13(S)-HPODE is a linoleic acid metabolite that acts as an EGFR activator. It has demonstrated significant biological activity in promoting cell proliferation and may play a role in various signaling pathways associated with cancer progression and inflammation. This compound is valuable for research into mechanisms of cancer biology and the development of therapeutic strategies targeting the EGFR pathway.

Cat. No.

A28939

CAS No.

187724-61-4

PKI-166

PKI-166 is a selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, demonstrating potent activity with an IC50 of 0.7 nM. It exhibits oral bioavailability and is utilized in research focused on cancer therapies that target aberrant EGFR signaling pathways. PKI-166 serves as a valuable tool for investigating the role of EGFR in tumorigenesis and evaluating the efficacy of EGFR-targeted treatments in various cancer models.

Cat. No.

A28940

CAS No.

1275595-86-2

Selatinib

Selatinib is a reversible and orally bioavailable dual inhibitor of epidermal growth factor receptor (EGFR) and ErbB2, demonstrating IC50 values of 13 nM and 22.5 nM, respectively. This compound exhibits significant anticancer activity, making it a valuable tool for research in targeted cancer therapies and studies focused on EGFR and ErbB2 signaling pathways.

Cat. No.

A28941

CAS No.

3031336-58-7

PROTAC EGFR degrader 2

PROTAC EGFR Degrader 2 is a highly effective small molecule that targets the epidermal growth factor receptor (EGFR) for degradation via the PROTAC mechanism. It demonstrates significant antiproliferative activity with an IC50 of 4.0 nM, along with robust EGFR degradation activity, exhibiting a DC50 of 36.51 nM. This compound is suitable for applications in cancer research, particularly in exploring EGFR-related pathways and developing nitroreductase (NTR)-responsive PROTAC systems.

Cat. No.

A28942

CAS No.

2064269-82-3

Pruvonertinib

Synonyms: YK-029A

Pruvonertinib is an orally active inhibitor specifically targeting mutant forms of the epidermal growth factor receptor (EGFR), including the T790M mutation and exon 20 insertions. This compound has demonstrated significant antitumor activity, leading to tumor regression in patient-derived xenograft models driven by EGFR exon 20 insertions. Pruvonertinib is a valuable reagent for research in cancer biology, particularly in studies focused on resistant mutations in lung cancer therapeutics.

Cat. No.

A28944

CAS No.

944258-89-3

Simotinib

Simotinib is a selective, orally bioavailable inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, with an IC50 value of 19.9 nM. This compound exhibits significant antineoplastic activity, making it a valuable tool for cancer research. Simotinib is primarily utilized in studies investigating the molecular mechanisms of EGFR signaling and the development of targeted therapies for EGFR-dependent tumors.

Cat. No.

A28945

CAS No.

2882845-50-1

PROTAC EGFR degrader 4

PROTAC EGFR Degrader 4 is a highly selective PROTAC designed to target mutant epidermal growth factor receptor (EGFR) variants. It effectively induces the degradation of EGFR del19 and the EGFR L858R/T790M double mutant, with DC50 values of 0.51 nM and 126 nM, respectively. This compound demonstrates significant growth inhibition in HCC827 and H1975 cell lines, exhibiting IC50 values of 0.83 nM and 203.1 nM. The degradation of EGFR is associated with autophagy, highlighting its potential in cancer research and therapeutic applications.

Cat. No.

A28946

CAS No.

945830-38-6

EGFR Protein Tyrosine Kinase Substrate

EGFR Protein Tyrosine Kinase Substrate serves as a substrate for the Epidermal Growth Factor Receptor (EGFR), facilitating the study of EGFR-mediated signaling pathways. This substrate is essential for investigating the catalytic activity of EGFR and its role in cellular processes such as proliferation and differentiation. It is particularly useful in research applications focusing on cancer biology, targeted therapies, and the development of EGFR inhibitors.

Cat. No.

A28948

CAS No.

1421680-54-7

Cys-GE11

Cys-GE11 is a cysteine-modified peptide that targets the epidermal growth factor receptor (EGFR). This peptide can be conjugated via its thiol group, enabling the formation of targeted polymeric constructs to improve drug delivery efficacy. Cys-GE11 demonstrates enhanced enrichment of therapeutic agents at tumor sites, particularly in EGFR-overexpressing cells, such as SMMC-7721. Its utilization in research highlights its potential for applications in targeted cancer therapy with minimal toxicity.

Cat. No.

A28949

CAS No.

2254805-44-0

BBT-176

BBT-176 is a potent oral inhibitor of the epidermal growth factor receptor (EGFR). It demonstrates significant inhibitory activity against various EGFR C797S mutant cell lines, making it a valuable tool for investigating resistance mechanisms in cancer therapy. This compound is widely utilized in cancer research to explore alternative treatment strategies targeting EGFR-related pathways.

Cat. No.

A29087

CAS No.

3060883-16-8

EGFR-IN-197

EGFR-IN-197 is a potent inhibitor of the Epidermal Growth Factor Receptor (EGFR), displaying IC50 values of 19.5 nM and 12.0 nM against the EGFRL858R/T790M and EGFRL858R/T790M/C797S mutations, respectively. This compound effectively arrests the cell cycle in the G2/M phase, inhibiting proliferation, colony formation, and migration of NCI-H1975 cells. Additionally, EGFR-IN-197 disrupts anti-apoptotic signaling pathways, induces DNA damage, and activates pro-apoptotic pathways, thereby triggering apoptosis. Its properties make it a valuable reagent for research focused on non-small cell lung cancer (NSCLC).

Cat. No.

A30311

CAS No.

1044040-56-3

Famitinib

Synonyms: SHR1020

Famitinib is a potent multi-targeted kinase inhibitor that primarily targets c-kit, VEGFR-2, and PDGFRβ, with IC50 values of 2.3 nM, 4.7 nM, and 6.6 nM, respectively. This orally active compound demonstrates significant antitumor activity in human gastric cancer cells and xenograft models. Famitinib also induces apoptosis, making it a valuable tool for research in cancer therapeutics and signaling pathways.

Cat. No.

A30828

CAS No.

3055550-22-3

EGFR-IN-86

EGFR-IN-86 is a potent EGFR inhibitor, exhibiting an IC50 of 1.5 nM. It demonstrates significant biological activity against glioblastoma by inducing apoptosis and causing cell cycle arrest in the G2/M phase in U87 cells. This compound serves as a valuable tool for research focused on targeting EGFR in cancer therapy.