Catalog No.
Product Name
Application
Product Information
Citations
-
EGFR inhibitor
Chrysophanic acid (Chrysophanol) blocks proliferation of colon cancer cells by inhibiting EGFR/mTOR pathway. -
EGFR, PKA,PKC inhibitor
Daphnetin is a coumarin analog that acts as an inhibitor of several protein kinases. It inhibits EGFR kinase (IC50 = 7.67 μM), PKA (IC50 = 9.33 μM), and PKC (IC50 = 25 μM), in vitro. The inhibition of EGFR kinase by daphnetin was competitive to ATP and non-competitive to the peptide substrate. Also acts as a potent antioxidant and anti-malarial agent. -
c-kit/VEGFR/PDGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR/HER2/TS Inhibitor
EGFR/HER2/TS-IN-1 is a selective inhibitor targeting EGFR, HER2, and thymidylate synthase (TS) with IC50 values of 0.203 μM, 0.088 μM, and 0.168 μM, respectively. This compound is effective in inducing apoptosis in MCF7 breast cancer cells, making it a valuable tool for cancer research. Its ability to simultaneously inhibit multiple targets renders it a promising candidate for exploring therapeutic strategies in malignancies characterized by overactive EGFR and HER2 signaling pathways. -
EGFR Inhibitor
EGFR-IN-150 is a potent inhibitor of the epidermal growth factor receptor (EGFR), effectively blocking phosphorylation of mutant EGFR and downstream AKT signaling, leading to antitumor activity. This compound demonstrates an IC50 of 0.386 μM in the non-small cell lung cancer (NSCLC) cell line H1975, significantly reducing colony formation and migration in both H1975 and A549 cells while promoting apoptosis. Furthermore, EGFR-IN-150 exhibits substantial tumor growth suppression in the H1975 cell-derived xenograft (CDX) mouse model, making it a valuable tool for research focused on non-small cell lung cancer. -
EGFR Inhibitor
Erbstatin is an inhibitor of the epidermal growth factor receptor (EGFR), targeting its kinase activity to impede downstream signaling pathways. This compound exhibits significant antineoplastic properties, making it a valuable reagent in cancer research. Erbstatin is utilized in studies investigating the role of EGFR in tumor progression and response to therapy, providing insights into potential treatment strategies for EGFR-mediated malignancies. -
EGFR2 Inhibitor
EGFR-IN-105 is a selective inhibitor of the EGFR2 receptor, with an IC50 value of 0.68 μM. This compound demonstrates significant anticancer activity by inducing apoptosis in cancerous cells, making it a valuable tool for investigating therapeutic strategies in pancreatic cancer research. Its specificity and potency position it as an important reagent for studies focused on targeting EGFR-related pathways in oncology. -
EGFR Inhibitor
EGFR-IN-45 is a potent inhibitor of the epidermal growth factor receptor (EGFR) with IC50 values of 0.4 µM for EGFR and 1.6 µM for CDK2. Additionally, it demonstrates inhibitory activity against Topoisomerase I and Topoisomerase II. This compound effectively induces apoptosis and arrests cancer cells in the pre-G1 phase, making it a valuable tool for cancer research and therapeutic studies targeting EGFR-related pathways. -
EGFR Inhibitor
Avitinib maleate dihydrate is a potent, irreversible, orally active selective inhibitor of epidermal growth factor receptor (EGFR). It exhibits high affinity, with IC50 values of 0.18 nM for both EGFR L858R and EGFR T790M mutations, as well as 7.68 nM for wild-type EGFR. In addition to its EGFR inhibition, Avitinib maleate dihydrate functions as a Bruton’s tyrosine kinase (BTK) inhibitor, promoting apoptosis in mantle cell lymphoma by inhibiting BTK phosphorylation. Its diverse targeting capabilities make it valuable for cancer research applications. -
EGFR Inhibitor
EGFR-IN-51 is a potent inhibitor of the epidermal growth factor receptor (EGFR), exhibiting IC50 values of 0.493 µM for wild-type EGFR, 102.60 µM for the L858R-TK mutation, and 461.63 µM for the T790M-TK mutation. This compound demonstrates significant cytotoxic activity against various cancer cell lines, effectively inducing apoptosis. EGFR-IN-51 is applicable in research focused on targeted cancer therapies and elucidating the role of EGFR signaling in tumorigenesis. -
EGFR Inhibitor
EGFR-IN-141 is a potent inhibitor of the epidermal growth factor receptor (EGFR), demonstrating an IC50 of 2.67 nM. This compound exhibits significant cytotoxicity in A549 lung cancer cells, with an IC50 of 13.75 μM. EGFR-IN-141 has been shown to induce apoptosis and cause mitochondrial membrane depolarization, highlighting its potential for antitumor efficacy in cancer research applications. -
EGFR Inhibitor
EGFR-IN-172 is a selective epidermal growth factor receptor (EGFR) inhibitor that effectively disrupts the proliferation of non-small cell lung cancer (NSCLC) cells harboring L858R, T790M, and C797S drug-resistant mutations. This compound acts by inhibiting EGFR phosphorylation, leading to cell cycle arrest and apoptosis in affected cells. EGFR-IN-172 serves as a valuable tool for research focused on NSCLC treatment and the development of targeted cancer therapies. -
EGFR/FAK Inhibitor
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. -
EGFRvIII Epitope
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFRT790M/L858R Inhibitor
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. -
EGFR-TKI
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR/HER2 Inhibitor
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. -
EGFR/BRAFV600E Inhibitor
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. -
EGFR Inhibitor
EGFR-IN-88 is a selective epidermal growth factor receptor (EGFR) inhibitor with an IC50 of 87 nM. The compound demonstrates cytotoxic effects on A549 cells, exhibiting an IC50 of 3.902 μM, and induces apoptosis in these cells. This compound is valuable for research focused on cancer therapies that target EGFR signaling pathways. -
EGFR Inhibitor
EGFR-IN-26 is a selective inhibitor of the epidermal growth factor receptor (EGFR), derived from patent WO2019162323A1, compound I-028. This compound significantly impedes EGFR activity, making it a valuable tool for investigating its role in cancer biology. It is applicable in cancer research, particularly in studies focused on targeting EGFR signaling pathways to develop novel therapeutic strategies. -
EGFR inhibitor
CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. -
PKC inhibitor
PKC 412 is a broad spectrum protein kinase inhibitor. Inhibits conventional PKC isoforms α/β/γ, PDFRβ, VEGFR2, Syk, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1 and EGFR. Displays potent antitumor activity. -
ErbB inhibitor
ARRY-543 is a novel, oral ErbB family inhibitor that, unlike approved ErbB inhibitors, targets all members of the ErbB family, including ErbB3, either directly or indirectly, and has potential advantages in treating tumors that signal through multiple ErbB family members. -
EGFR inhibitor
CO-1686 is a novel, oral, targeted covalent (irreversible) inhibitor of the cancer-causing mutant forms of epidermal growth factor receptor (EGFR) currently being studied for the treatment of non-small cell lung cancer (NSCLC). -
EGFR inhibitor
CL-387785 is an irreversible inhibitor of EGFR with IC50 of 370+/-120 pM; is able to overcome resistance caused by the T790M mutation on a functional level. -
EGFR/T790M inhibitor
HS-10296 hydrochloride is an orally available and third-Generation inhibitor of epidermal growth factor receptor (EGFR)-activating mutations and T790M-resistant mutation with limited activity against wild-type EGFR. -
HER1/HER2 inhibitor
BMS-599626 (AC480) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. -
EGFR inhibitor
Nazartinib mesylate (EGF816 mesylate) is a novel, covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min?1 on EGFR(L858R/790M) mutant, respectively. -
EGFR inhibitor
Nazartinib S-enantiomer (EGF816 S-enantiomer) is the less active S-enantiomer of Nazartinib. Nazartinib (EGF816) is an EGFR inhibitor.
