EGFR/HER2

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.

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.

Cat. No.

A32329

CAS No.

2413958-04-8

EGFR kinase inhibitor 1

EGFR Kinase Inhibitor 1 is a selective inhibitor targeting the epidermal growth factor receptor (EGFR), exhibiting IC50 values of 37 nM for wild-type, 1.7 nM for L858R/T790M, and greater than 300 nM for L858R/T790M/C797S mutant variants. This compound induces apoptosis and promotes cell cycle arrest at the G0/G1 phase, effectively inhibiting cell motility. Its strong antiproliferative and anti-tumor activities make it a valuable tool for research in cancer biology, particularly in studies related to EGFR-driven malignancies.

Cat. No.

A32330

CAS No.

2477726-83-1

EGFR-IN-56

EGFR-IN-56 is a potent inhibitor of the epidermal growth factor receptor (EGFR), demonstrating IC50 values of 541.7 nM and 132.1 nM against the EGFRT790M and EGFRT790M/L858R mutations, respectively. This compound significantly disrupts cell cycle progression by blocking cancer cells in the G2/M phase and facilitating late apoptosis. It is suitable for studies examining the therapeutic potential of EGFR inhibition in cancer research.

Cat. No.

A32413

CAS No.

2492382-37-1

EGFR-IN-57

EGFR-IN-57 is a potent EGFR tyrosine kinase inhibitor with an IC50 of 0.054 µM, demonstrating significant inhibitory activity against additional targets including VEGFR-2, CK2α, topoisomerase IIβ, and tubulin polymerization, with respective IC50 values of 0.087, 0.171, 0.130, and 3.61 µM. This compound effectively induces cell cycle arrest at the G2/M and pre-G1 phases, promoting apoptosis in cancer cells. EGFR-IN-57 is utilized in research applications focused on cancer therapy, specifically targeting EGFR signaling pathways and elucidating mechanisms of tumor growth and resistance.

Cat. No.

A32416

CAS No.

1970269-96-5

EGFR/microtubule-IN-1

EGFR/microtubule-IN-1 is a dual inhibitor targeting epidermal growth factor receptor (EGFR) and tubulin. It exhibits an IC50 of 10.66 nM for EGFR inhibition, effectively reducing phosphorylation levels of EGFR, AKT, and ERK. Additionally, this compound disrupts tubulin polymerization and induces apoptosis, making it a valuable tool for cancer research and studies focused on cell signaling pathways and microtubule dynamics.

Cat. No.

A32449

CAS No.

2463197-87-5

EGFR-IN-152

EGFR-IN-152 is a highly selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, demonstrating significant inhibitory activity against the EGFR L858R/T790M/C797S mutant isoforms, with an IC50 of 40 nM. This compound effectively induces G0/G1 phase cell cycle arrest and apoptosis, leading to the inhibition of colony formation and cell proliferation in non-small cell lung cancer (NSCLC) models. EGFR-IN-152 serves as a valuable tool for research focusing on NSCLC and novel therapeutic strategies targeting EGFR mutations.

Cat. No.

A32452

CAS No.

3020681-05-1

EGFR-IN-97

EGFR-IN-97 is a selective inhibitor of the epidermal growth factor receptor (EGFR). This compound demonstrates potent inhibitory activity against Ba/F3 cells expressing EGFR mutations, specifically L858R/T790M/C797S and Del19/T790M/C797S, with IC50 values of 0.42 μM and 0.41 μM, respectively. Additionally, EGFR-IN-97 effectively induces apoptosis in NCI-H1975 cells harboring the EGFR L858R/T790M/C797S mutations at a concentration of 0.8 μM. This reagent is valuable for research focused on targeted therapies in EGFR-mutant cancers.

Cat. No.

A32467

CAS No.

2820126-50-7

EGFR/HER2-IN-6

EGFR/HER2-IN-6 is a potent inhibitor of EGFR and HER2 kinases, as well as dihydrofolate reductase (DHFR), with IC50 values of 0.122 μM, 0.078 μM, and 0.585 μM, respectively. This compound displays significant anticancer activity across various cancer cell lines, demonstrating a favorable safety profile and selectivity. EGFR/HER2-IN-6 is valuable for research on cancer therapeutics targeting these critical pathways.

Cat. No.

A32473

CAS No.

2492429-45-3

EGFR/BRAFV600E-IN-1

EGFR/BRAFV600E-IN-1 is a potent dual inhibitor targeting EGFR and the BRAFV600E mutation, with IC50 values of 0.08 µM and 0.15 µM, respectively. This compound effectively induces apoptosis and induces cell cycle arrest in the pre-G1 and G2/M phases. Additionally, it demonstrates significant antiproliferative activity against A-549, MCF-7, Panc-1, and HT-29 cell lines, with IC50 values of 1.2 µM, 0.79 µM, 1.3 µM, and 1.23 µM, respectively, making it valuable for cancer research focused on these targets.