EGFR/HER2

Cat. No.

A31053

CAS No.

1323883-62-0

T-1-PMPA

T-1-PMPA is a potent inhibitor of the epidermal growth factor receptor (EGFR), demonstrating significant apoptotic effects. This compound effectively targets both wild-type EGFR (EGFRWT) and the EGFR 790M mutation, exhibiting IC50 values of 86 nM and 561.73 nM, respectively. T-1-PMPA is suitable for research applications focused on cancer biology and therapeutic efficacy in EGFR-related pathways.

Cat. No.

A31106

CAS No.

3034649-73-2

EGFR-IN-47

EGFR-IN-47 is a potent orally active inhibitor of the EGFR L858R/T790M/C797S mutations, with an IC50 of 0.01 μM. This compound effectively induces cell cycle arrest and promotes apoptosis in cancer cells. EGFR-IN-47 holds significant potential for research applications related to non-small cell lung cancer (NSCLC).

Cat. No.

A31135

CAS No.

3042104-73-1

EGFR-IN-78

EGFR-IN-78 is a reversible inhibitor of the EGFR variant C797S-TK, classified as a 2-aminopyrimidine derivative. This compound induces apoptosis and exhibits significant anti-proliferative activity by inhibiting EGFR phosphorylation. Additionally, EGFR-IN-78 effectively arrests the cell cycle at the G2/M phase, making it a valuable tool for research applications focused on targeted cancer therapies.

Cat. No.

A31148

CAS No.

3053485-72-3

EGFR-TK-IN-4

EGFR-TK-IN-4 is a potent and selective inhibitor of the epidermal growth factor receptor tyrosine kinase (EGFR-TK). It has been demonstrated to induce apoptosis in cancer cells and exhibits significant antitumor activity. This compound is suitable for studying EGFR signaling pathways and developing targeted therapies in oncology research.

Cat. No.

A31163

CAS No.

2470908-90-6

YS-363

YS-363 is a potent and selective orally active inhibitor of the epidermal growth factor receptor (EGFR), exhibiting IC50 values of 0.96 nM for wild-type and 0.67 nM for the L858R mutant form. This compound effectively induces G0/G1 cell cycle arrest and promotes apoptosis in target cells. YS-363 is valuable for research applications focused on cancer therapeutics and the molecular mechanisms of EGFR signaling.

Cat. No.

A31326

CAS No.

2998928-68-8

Os30

Os30 is a potent fourth-generation EGFR inhibitor specifically targeting the EGFRC797S-TK mutation. With IC50 values of 18 nM and 113 nM for EGFRDel19/T790M/C797S TK and EGFRL858R/T790M/C797S TK, respectively, Os30 effectively inhibits EGFR phosphorylation, induces G1 phase cell cycle arrest, and triggers apoptosis in KC-0116 (BaF3-EGFRDel19/T790M/C797S) cells. This compound demonstrates significant antitumor activity in non-small cell lung cancer (NSCLC) harboring the EGFRC797S mutation, making it a valuable tool for cancer research and therapeutic exploration.

Cat. No.

A31336

CAS No.

1639040-95-1

pan-HER-IN-2

pan-HER-IN-2 is a reversible, orally active pan-HER inhibitor targeting multiple receptor tyrosine kinases, with IC50 values of 0.72 nM for EGFR, 2.0 nM for HER4, 8.2 nM for EGFRT790M/L858R, and 75.1 nM for HER2. This compound effectively induces apoptosis and exhibits significant antitumor activities. pan-HER-IN-2 is suitable for research applications focused on cancer therapy and the exploration of targeted treatments for HER family receptor-positive tumors.

Cat. No.

A31500

CAS No.

184475-56-7

Gefitinib dihydrochloride

Synonyms: ZD 1839 dihydrochloride

Gefitinib dihydrochloride is a potent and selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, exhibiting an IC50 of 33 nM. This compound effectively inhibits EGF-stimulated tumor cell proliferation (IC50 of 54 nM) and prevents EGFR autophosphorylation, thereby blocking downstream signaling pathways. Gefitinib dihydrochloride is valuable for cancer research, particularly in the study of lung and breast cancers, due to its ability to induce autophagy and promote apoptosis in tumor cells.

Cat. No.

A31501

CAS No.

1626387-81-2

Zorifertinib hydrochloride

Synonyms: AZD3759 hydrochloride

Zorifertinib hydrochloride is a potent orally active inhibitor of the epidermal growth factor receptor (EGFR), demonstrating IC50 values of 0.3 nM, 0.2 nM, and 0.2 nM against wild-type EGFR, EGFR L858R, and EGFR exon 19 deletion variants, respectively. This compound is capable of inducing apoptosis in cancer cells and exhibits significant antitumor activity. Zorifertinib hydrochloride is primarily utilized in research related to non-small cell lung cancer (NSCLC) and hepatocellular carcinoma (HCC).

Cat. No.

A31584

CAS No.

1256377-67-9

Famitinib malate

Synonyms: SHR1020 malate

Famitinib malate is an orally active, multi-targeted kinase inhibitor primarily targeting c-kit, VEGFR-2, and PDGFRβ, with IC50 values of 2.3 nM, 4.7 nM, and 6.6 nM, respectively. This compound induces cell apoptosis and demonstrates significant anti-tumor activity in human gastric cancer cells and xenograft models. Famitinib malate is a valuable tool for research into cancer therapies and mechanisms of action.

Cat. No.

A31650

CAS No.

1350545-09-3

SKLB188

SKLB188 is a potent and orally active inhibitor of the epidermal growth factor receptor (EGFR), exhibiting an IC50 of 5 nM. This compound effectively suppresses both MEK/Erk and Akt/mTOR signaling pathways, leading to reduced proliferation of head and neck squamous cell carcinoma (HNSCC) and inducing caspase-dependent apoptosis. SKLB188 is a valuable reagent for research focused on EGFR-overexpressing solid tumors.

Cat. No.

A31659

CAS No.

2529891-44-7

EGFR-IN-59

EGFR-IN-59 is an epidermal growth factor receptor (EGFR) inhibitor with an IC50 of 190 nM, demonstrating apoptosis-inducing properties. This compound exhibits significant cytotoxicity against non-small cell lung cancer cell lines (A549) with an IC50 of 8.62 µM, while maintaining a lower cytotoxic effect on normal lung fibroblasts (WI38) at 52.6 µM. EGFR-IN-59 is a valuable tool for investigating various cancers, including non-small cell lung cancer (NSCLC), head and neck cancer, breast cancer, and colorectal cancer.

Cat. No.

A31699

CAS No.

1639040-94-0

pan-HER-IN-1

pan-HER-IN-1 is an irreversible pan-HER inhibitor that targets multiple human epidermal growth factor receptors (HER) with IC50 values of 0.38 nM for EGFR, 1.6 nM for HER4, 2.2 nM for EGFRT790M/L858R, and 3.5 nM for HER2. This compound effectively induces apoptosis and exhibits significant antitumor activity, making it a valuable tool for cancer research and therapeutic applications aimed at HER-driven malignancies.

Cat. No.

A31763

CAS No.

2393787-80-7

GLUT1/EGFR-IN-1

GLUT1/EGFR-IN-1 is a potent inhibitor of both the GLUT1 transporter and the EGFR tyrosine kinase. By targeting the ATP-binding site of EGFR and concurrently inhibiting GLUT1-mediated energy metabolism, GLUT1/EGFR-IN-1 effectively reduces ATP levels, mitochondrial membrane potential, and intracellular lactic acid, while also preventing EGFR nuclear translocation. This compound is applicable in research focusing on nasopharyngeal carcinoma (NPC) and triple-negative breast cancer (TNBC).

Cat. No.

A31838

CAS No.

2764772-88-3

EGFR-IN-46

EGFR-IN-46 is a potent dual inhibitor targeting the epidermal growth factor receptor (EGFR) and focal adhesion kinase (FAK), with IC50 values of 20.17 nM and 14.25 nM, respectively. This compound effectively inhibits cancer cell proliferation and induces apoptotic pathways in these cells. EGFR-IN-46 is designed for research applications focused on cancer biochemistry and therapeutic development.

Cat. No.

A31871

CAS No.

916850-24-3

EGFRvIII peptide

EGFRvIII peptide is a synthetic epitope derived from the EGFRvIII variant, specifically designed to bind to MHC I molecules. This peptide is known to induce apoptosis and elicit targeted immune responses against glioblastoma, particularly when used in conjunction with Flagellin B. It is a valuable tool for research in cancer immunotherapy and the development of personalized medicine approaches for glioblastoma treatment.

Cat. No.

A31882

CAS No.

2699877-43-3

EGFR-IN-60

EGFR-IN-60 is a potent inhibitor of the epidermal growth factor receptor (EGFR), specifically targeting EGFRWT, EGFRT790M, EGFRL858R, and JAK3 with IC50 values of 83, 26, 53, and 69 nM, respectively. This compound effectively suppresses the proliferation of H1975 cells with the EGFRT790M mutation (IC50=1.32 µM) while yielding less potency against A431 cells expressing EGFRWT (IC50=4.96 µM). With favorable oral bioavailability, EGFR-IN-60 demonstrates significant antitumor activity, promoting cell death via apoptosis as indicated by an increased Bax/Bcl-2 ratio. This makes it a valuable candidate for research into targeted therapies for EGFR-related cancers.

Cat. No.

A31887

CAS No.

535959-77-4

Cyclic(YCDGFYACYMDV)

Cyclic(YCDGFYACYMDV) is a selective inhibitor of the HER2 signaling pathway, exhibiting significant anti-cancer activity. This compound self-assembles into nanoparticles in aqueous environments and converts into nanofibers upon specific binding to HER2 on tumor cells, effectively disrupting HER2 dimerization and downstream signaling, thereby inducing apoptosis. Its inhibitory effects on HER2-positive breast cancer have been validated in murine xenograft models, making it a valuable tool for cancer research and therapeutic development.

Cat. No.

A31920

CAS No.

2890261-65-9

EGFR-IN-62

EGFR-IN-62 is a potent and reversible inhibitor of the epidermal growth factor receptor (EGFR) kinase, demonstrating IC50 values of 10 nM for the L858R/T790M mutation, 29 nM for wild-type EGFR, and 242 nM for the L858R/T790M/C797S mutation. This compound exhibits significant antiproliferative effects on human lung cancer cell lines A549 and H1975, with IC50 values of 2.53 μM and 1.56 μM, respectively. Furthermore, EGFR-IN-62 promotes dose-dependent apoptosis, induces G1/G0 phase arrest, and inhibits cell motility, making it a valuable tool for research in cancer biology and targeted therapies.

Cat. No.

A31926

CAS No.

454436-75-0

EGFR-IN-52

EGFR-IN-52 is a potent inhibitor of the epidermal growth factor receptor (EGFR) with IC50 values of 0.358 µM for wild-type EGFR, 86.02 µM for the L858R-TK variant, and 432.67 µM for the T790M-TK resistance mutant. This compound exhibits significant cytotoxicity against various cancer cell lines and is known to induce apoptosis. EGFR-IN-52 is valuable for research applications focusing on targeted cancer therapies and the study of EGFR signaling pathways.

Cat. No.

A31952

CAS No.

3031812-65-1

EGFR-IN-3

EGFR-IN-3 is a selective inhibitor of the epidermal growth factor receptor (EGFR), demonstrating an IC50 of 0.32 µM against EGFR wild-type kinase. This compound exhibits significant cytotoxic effects on various cancer cell lines and promotes apoptosis, making it a valuable tool for studies related to cancer biology and therapeutic development targeting EGFR signaling pathways.

Cat. No.

A32033

CAS No.

2955607-40-4

EGFR T790M/L858R-IN-2

EGFR T790M/L858R-IN-2 is a selective inhibitor of the EGFR T790M and L858R mutants, exhibiting IC50 values of 3.5 nM and 1290 nM for these targets, respectively. This compound effectively reduces the phosphorylation of EGFR, AKT, and ERK1/2, subsequently inducing apoptosis and causing cell cycle arrest in the G1 phase. EGFR T790M/L858R-IN-2 demonstrates significant anti-cancer activity, making it a valuable tool for research in targeted therapies for lung cancer and other malignancies associated with these mutations.

Cat. No.

A32044

CAS No.

1451370-01-6

TAS-121

TAS-121 is a selective, covalent third-generation mutant EGFR-tyrosine kinase inhibitor (EGFR-TKI) that targets various EGFR mutations, including L858R (IC50=1.7 nM), Ex19del (IC50=2.7 nM), L858R/T790M (IC50=0.56 nM), and Ex19del/T790M (IC50=1.1 nM), as well as wild-type EGFR (IC50=8.2 nM). It also exhibits inhibitory activity against HER2 and HER4 with IC50s of 110 and 2.6 nM, respectively. TAS-121 effectively inhibits EGFR phosphorylation and downstream signaling pathways, leading to reduced cell proliferation and induction of apoptosis. Its antitumor efficacy has been demonstrated in xenograft models utilizing SW48 (EGFR G719S) and NCI-H1975 (EGFR L858R/T790M) cell lines.

Cat. No.

A32167

CAS No.

3035639-05-2

EGFR-IN-117

EGFR-IN-117 is a potent EGFR inhibitor designed to target mutated forms of the epidermal growth factor receptor. It exhibits significant inhibitory activity against a range of EGFR mutant cell lines, including H1975, PC-9, BaF3-EGFRL858R/T790M/C797S, and BaF3–C797S/Del19/T790M, with IC50 values of 13 nM, 19 nM, 1.2 nM, and 1.3 nM, respectively. In addition to its antiproliferative effects, EGFR-IN-117 induces apoptosis and demonstrates antitumor efficacy in preclinical mouse models, making it a valuable tool for cancer research.

Cat. No.

A32320

CAS No.

3031099-34-7

EGFR-IN-161

EGFR-IN-161 is a potent and reversible inhibitor targeting L858R/T790M/C797S mutant EGFR kinases, demonstrating an IC50 of 0.87 nM. This compound effectively induces apoptosis, causes G1-phase cell cycle arrest, and inhibits migration in tumor cells, making it a valuable tool for cancer research focused on EGFR mutations. Its specificity and efficacy provide significant potential in the study of targeted therapies for resistant forms of non-small cell lung cancer.