EGFR/HER2

Cat. No.

A28603

CAS No.

2411874-83-2

LDC0496

LDC0496 is a potent and selective inhibitor of the epidermal growth factor receptor (EGFR). It demonstrates strong inhibitory activity against both EGFR and Her2 exon 20 insertion mutations, while maintaining selectivity for wild-type EGFR and demonstrating minimal cross-reactivity within the kinome. This compound is valuable for research applications focused on targeted therapies in cancers associated with EGFR mutations.

Cat. No.

A28604

CAS No.

1226549-39-8

EGFR-IN-9

EGFR-IN-9 is a potent inhibitor of the epidermal growth factor receptor (EGFR) kinase, exhibiting IC50 values of 7 nM for wild-type EGFR and 28 nM for the double mutant EGFR (L858R/T790M). This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research, particularly in studies focusing on EGFR-related pathways and mutations. It is suitable for investigations into therapeutic strategies targeting EGFR in various cancer models.

Cat. No.

A28605

CAS No.

2910858-34-1

Antiproliferative agent-34

Antiproliferative agent-34 is a selective inhibitor targeting EGFR L858R/T790M with an IC50 of 177 nM, while exhibiting inhibition of EGFR WT at 1567 nM. This compound also effectively inhibits several kinases, including JAK2, ROS1, FLT3, FLT4, and PDGFRα with IC50 values ranging from approximately 30 nM to 226 nM. Antiproliferative agent-34 demonstrates significant anti-proliferative activity in H1975 and HCC827 cancer cell lines, with IC50 values below 40 nM under normoxic conditions, and enhanced potency of 4–6-fold under hypoxic conditions, making it a valuable tool for cancer research focused on targeted therapies.

Cat. No.

A28606

CAS No.

171179-37-6

BPIQ-II hydrochloride

Synonyms: PD 158294

BPIQ-II hydrochloride is a potent inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, exhibiting an IC50 value of 8 pM. This compound selectively targets EGFR while showing minimal interaction with various other tyrosine and serine/threonine kinases. In cellular studies, BPIQ-II effectively penetrates cells and specifically disrupts EGF-stimulated signal transduction by competitively binding to the ATP site of EGFR. This makes it a valuable tool for research into EGFR-related signaling pathways and targeted cancer therapies.

Cat. No.

A28607

CAS No.

439081-17-1

(R)-Afatinib

Synonyms: (R)-BIBW 2992

(R)-Afatinib is a potent and irreversible dual specificity inhibitor targeting the ErbB family, specifically EGFR and HER2. With IC50 values of 0.5 nM, 0.4 nM, 10 nM, and 14 nM for EGFR wild type, EGFR L858R, EGFR L858R/T790M, and HER2, respectively, this compound exhibits significant biological activity against these receptors. (R)-Afatinib is utilized in research focused on esophageal squamous cell carcinoma, non-small cell lung cancer, and gastric cancer, providing essential insights into targeted therapies.

Cat. No.

A28608

CAS No.

2568086-81-5

EGFR-IN-82

EGFR-IN-82 is a highly selective and orally bioavailable inhibitor of the epidermal growth factor receptor (EGFR), exhibiting IC50 values of 0.09 nM for the EGFRL858R/T790M/C797S mutant and 0.06 nM for EGFRDel19/T790M/C797S. This compound demonstrates significant anti-proliferative effects and inhibits tumor formation in nude mice models. EGFR-IN-82 is a valuable tool for research into non-small cell lung cancer, particularly in studies focused on resistant EGFR mutations.

Cat. No.

A28609

CAS No.

2360839-74-1

ER121

Synonyms: SGI-078

ER121 is a selective ErbB2 kinase inhibitor that exhibits oral bioavailability and non-toxic properties. It demonstrates potent antitumor activity, making it a valuable tool for the investigation of HER2-related breast cancer. Researchers can utilize ER121 to explore its effects on signaling pathways and evaluate potential therapeutic strategies in oncology.

Cat. No.

A28610

CAS No.

2229835-58-7

EGFR/HER2-IN-19

EGFR/HER2-IN-19 is a potent dual inhibitor of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2). This compound exhibits significant anti-proliferative activity in cancer cells driven by EGFR and HER2 signaling pathways. It serves as a valuable tool for research applications focused on understanding and targeting EGFR/HER2-mediated tumorigenesis.

Cat. No.

A28611

CAS No.

1240322-54-6

Antiproliferative agent-54

Antiproliferative agent-54 is a potent EGFR inhibitor that targets multiple kinases, including ABL WT, B-RAF, HCK, LYN A, and SRC, with IC50 values ranging from 6 to 50 nM. This compound effectively reduces the proliferation of various cancer cell lines and shows significant inhibitory effects on human umbilical vein endothelial cells (HUVEC) and HepG2 cells, with EC50 values of 34 and 38 nM, respectively. Antiproliferative agent-54 also demonstrates favorable pharmacokinetic properties in rat models, supporting its potential for further research applications in cancer therapy.

Cat. No.

A28612

CAS No.

2414056-35-0

HER2-IN-14

HER2-IN-14 is a potent HER2 inhibitor, exhibiting an IC50 value of 18 nM. Additionally, it demonstrates activity against wild-type EGFR with an IC50 of 6.3 μM. This compound is valuable for investigating HER2-mediated signaling pathways and is relevant in the context of cancer research, particularly in studies targeting breast cancer and other HER2-overexpressing malignancies.

Cat. No.

A28614

CAS No.

2989904-86-9

EGFR-IN-204

EGFR-IN-204 is a HER2 exon 20 mutation inhibitor with selective action against wild-type EGFR. This compound demonstrates significant antiproliferative effects on cells that are reliant on the HER2 exon 20 YVMA insertion mutation, while exhibiting strong selectivity for wild-type HER2. EGFR-IN-204 is particularly relevant for research focusing on non-small cell lung cancer and the treatment of HER2-driven malignancies.

Cat. No.

A28616

CAS No.

2765573-34-8

EGFR-IN-18

EGFR-IN-18 is a selective inhibitor of the epidermal growth factor receptor (EGFR), specifically targeting the L858R/T790M/C797S mutant variant with a potency of 4.9 nM. In contrast, it exhibits reduced activity against wild-type EGFR at 47 nM. This compound is valuable for studying EGFR-driven cancer models and may facilitate the development of targeted therapies in oncology research.

Cat. No.

A28617

CAS No.

3785-90-8

Tyrphostin 8

Tyrphostin 8 is an inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, exhibiting an IC50 of 560 μM. Additionally, it acts as a GTPase inhibitor and can effectively inhibit the protein serine/threonine phosphatase calcineurin, with an IC50 of 21 μM. Tyrphostin 8 is utilized in research applications focusing on cancer biology, signal transduction pathways, and the regulation of cellular processes influenced by EGFR signaling.

Cat. No.

A28618

CAS No.

2882851-77-4

EGFR-IN-48

EGFR-IN-48 is a highly potent and orally active inhibitor of the epidermal growth factor receptor (EGFR), exhibiting IC50 values of 0.193 nM, 0.251 nM, and 10.4 nM against EGFR del19/TM/CS, EGFRLR/TM/CS, and EGFR wild-type, respectively. This compound effectively inhibits the proliferation of BaF3 cells harboring the EGFR del19/T790M/C797S mutation, as well as PC-9 cells with IC50s of 1.526 nM and 66.7 nM, respectively. EGFR-IN-48 is a valuable tool for research focused on cancer therapeutics, particularly in studies regarding EGFR mutation-related resistance mechanisms.

Cat. No.

A28619

CAS No.

2237230-21-4

EGFR/HER2-IN-12

EGFR/HER2-IN-12 is a selective dual inhibitor of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2). It demonstrates robust biological activity, achieving 81% inhibition of EGFR and 51% inhibition of HER2 at a concentration of 10 μM. This compound shows a low toxicity profile in cancer cell lines A431 and MDA-MB-361, making it a valuable tool for research in cancer biology and targeted therapy development.

Cat. No.

A28620

CAS No.

136904-69-3

2′-Thioadenosine

Synonyms: PD157432

2′-Thioadenosine is a selective and irreversible inhibitor of ErbB-1 and ErbB-2, demonstrating an IC50 of 45 µM for ErbB-2. Its primary mechanism involves the covalent modification of a cysteine residue at the active site of ErbB-1, leading to inactivation of the receptor. This compound is primarily employed in research applications focusing on cancer biology and targeted therapies where ErbB signaling pathways play a crucial role.

Cat. No.

A28622

CAS No.

733009-42-2

EGFR-IN-198

EGFR-IN-198 is a selective inhibitor of the epidermal growth factor receptor (EGFR), exhibiting subnanomolar irreversible inhibition. This compound covalently binds to the kinase domain of EGFR, effectively disrupting its autophosphorylation and downstream signaling pathways. EGFR-IN-198 is utilized in research focusing on cancer biology, particularly in studies investigating EGFR-driven tumors and potential therapeutic interventions targeting this pathway.

Cat. No.

A28623

CAS No.

1216920-18-1

BIBX 1382 dihydrochloride

BIBX 1382 dihydrochloride is a selective ErbB kinase inhibitor that exhibits notable antiviral activity. By inhibiting members of the ErbB kinase family, BIBX 1382 interferes with viral entry into host cells. This compound serves as a valuable tool for investigating the mechanisms of virus-host interactions and evaluating therapeutic interventions against a range of highly pathogenic viruses.

Cat. No.

A28624

CAS No.

2418549-33-2

EGFR-IN-53

EGFR-IN-53 is a potent inhibitor of the epidermal growth factor receptor (EGFR), exhibiting an IC50 of 8.264 µM. This compound demonstrates significant cytotoxic activity against various cancer cell lines, making it a valuable tool for cancer research. EGFR-IN-53 can be employed in studies investigating EGFR-mediated signaling pathways, therapeutic resistance, and potential combination therapies in oncology.

Cat. No.

A28626

CAS No.

3008611-00-2

EGFR-IN-90

EGFR-IN-90 is a potent orally active inhibitor targeting the epidermal growth factor receptor (EGFR). It demonstrates significant inhibitory activity against the EGFRL858R/T790M/C797S mutations, with an IC50 of 5.1 nM. Additionally, EGFR-IN-90 effectively reduces proliferation in the H1975-TM cell line associated with these mutations, exhibiting an IC50 of 0.05 μM. In vivo, it has been shown to inhibit tumor growth in the H1975-TM xenograft tumor model, making it a valuable tool for cancer research focused on EGFR-related pathways.

Cat. No.

A28629

CAS No.

3032113-20-2

EGFR-IN-91

EGFR-IN-91 is a selective inhibitor of the epidermal growth factor receptor (EGFR), effective against the EGFR L858R/C797S and EGFR exon 19 deletion/C797S mutants. This compound demonstrates significant anticancer activity by inducing tumor regression in patient-derived xenograft models, making it a valuable tool for research in localized and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutations. Additionally, EGFR-IN-91's ability to penetrate the blood-brain barrier suggests potential applications in treating brain metastases associated with NSCLC.

Cat. No.

A28630

CAS No.

144909-21-7

RG 14921

RG 14921 is a potent inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. This compound functions as a noncompetitive inhibitor, effectively blocking EGFR signaling pathways and CAMP-dependent kinase activity. RG 14921 is utilized in research applications focused on cancer biology, particularly in studies investigating the role of EGFR in tumorigenesis and therapeutic resistance.

Cat. No.

A28631

CAS No.

1538617-88-7

Simotinib hydrochloride

Simotinib hydrochloride is a selective EGFR tyrosine kinase inhibitor, demonstrating an IC50 of 19.9 nM. This compound exhibits potent antineoplastic activity, making it a valuable tool for cancer research and therapeutic development targeting EGFR-associated malignancies. Its oral bioavailability enhances its potential for in vivo studies.

Cat. No.

A28632

CAS No.

2172879-84-2

EGFR-IN-160

EGFR-IN-160 is a selective EGFR inhibitor, exhibiting IC50 values of 1.62 μM, 0.49 μM, and 0.98 μM against EGFRWT, EGFRT790M, and EGFRL858R/T790M/C797S variants, respectively. This compound effectively induces G2/M and S phase cell cycle arrest and apoptosis in NCI-H522 lung cancer cells, showcasing its potential as an anticancer agent. Additionally, EGFR-IN-160 demonstrates antioxidant properties, as evidenced by its IC50 values of 12.11 µM against DPPH and 8.89 µM against H2O2, further supporting its relevance in cancer research and therapeutic development.

Cat. No.

A28634

CAS No.

185039-99-0

PD 173955 analog 1

PD 173955 analog 1 is a selective inhibitor of the epidermal growth factor receptor (EGFR) kinase. This compound demonstrates significant antitumor activity and has been characterized for its toxicological effects. In silico studies have reported an IC50 value of 0.19 μM, indicating its efficacy in modulating EGFR-related signaling pathways, making it a valuable tool for cancer research and therapeutic investigations.