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Catalog No.
Product Name
Application
Product Information
Citations
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EGFR Inhibitor
JBJ-09-063 is a mutant-selective allosteric inhibitor targeting the epidermal growth factor receptor (EGFR). It exhibits potent inhibitory activity with IC50 values of 0.147 nM for EGFR L858R, 0.063 nM for EGFR L858R/T790M, 0.083 nM for EGFR L858R/T790M/C797S, and 0.396 nM for EGFR L747S. JBJ-09-063 effectively attenuates phosphorylation of EGFR, Akt, and ERK1/2, demonstrating its utility in both TKI-sensitive and resistant models. This compound is particularly valuable for studying EGFR-mutant lung cancer and exploring therapeutic strategies for treatment-resistant variants. -
EGFR Mutant Inhibitor
Mutated EGFR-IN-3 is a highly selective allosteric inhibitor targeting the mutant forms of epidermal growth factor receptor (EGFR), specifically EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S). It demonstrates potent ATP-competitive inhibition with IC50 values of 12 nM and 13 nM, respectively. This compound is valuable for research applications focused on understanding and treating cancers driven by these specific EGFR mutations. -
EGFR Inhibitor
EGFR-IN-17 is a potent and selective inhibitor of the epidermal growth factor receptor (EGFR), exhibiting an IC50 value of 0.0002 μM. It is specifically designed to address C797S-mediated resistance, making it a valuable tool for researchers investigating EGFR-related pathways in cancer. This compound is applicable for studies focusing on therapeutic strategies against resistant forms of malignancies driven by EGFR signaling. -
HER2/EGFR Inhibitor
GW2974 is a potent dual inhibitor of the human epidermal growth factor receptor 2 (HER2) and epidermal growth factor receptor (EGFR), with IC50 values of 0.007 μM and 0.016 μM, respectively. It effectively inhibits the proliferation of tumor cells in vitro, making it a valuable tool in cancer research. GW2974 is particularly relevant for studies focused on glioblastoma multiforme (GBM) and related malignancies. -
EGFR/ErbB2 Inhibitor
Tephrosin is a natural rotenoid that functions as an inhibitor of the epidermal growth factor receptor (EGFR) and ErbB2. It demonstrates significant antitumor activity by promoting the internalization and subsequent degradation of these receptors, thereby disrupting downstream signaling pathways involved in cellular proliferation and survival. This compound is useful in cancer research, particularly in studies focusing on targeted therapies for EGFR and ErbB2-overexpressing tumors. -
EGFR/AURKB Inhibitor
EGFR/AURKB-IN-1 is a dual inhibitor targeting Epidermal Growth Factor Receptor (EGFR) and Aurora Kinase B (AURKB), effectively blocking their phosphorylation with IC50 values of 0.07 µM and 1.1 µM, respectively. This compound binds to the hydrophobic region I and αC-helix out pocket of EGFR, as well as the back pocket of AURKB, thereby inhibiting tumor cell growth, division, and metastasis. EGFR/AURKB-IN-1 is suitable for comprehensive cancer research applications aimed at elucidating mechanisms of tumor progression and therapy resistance. -
EGFR Inhibitor
PF-6274484 is a highly selective inhibitor of the epidermal growth factor receptor (EGFR), with inhibitory constants (Kis) of 0.14 nM for the EGFR-L858R/T790M mutant and 0.18 nM for wild-type EGFR. This compound effectively inhibits autophosphorylation of EGFR-L858R/T790M in H1975 cells and wild-type EGFR in A549 cells, demonstrating IC50 values of 6.6 nM and 5.8 nM, respectively. PF-6274484 is valuable for researching targeted therapies in EGFR-driven cancers and elucidating signaling pathways linked to tumor proliferation. -
EGFR Inhibitor
Dosimertinib-d5 mesylate is a potent, orally active inhibitor of the epidermal growth factor receptor (EGFR). It effectively reduces the levels of phosphorylated EGFR and ERK proteins, demonstrating significant antiproliferative and anti-tumor activities. This compound is particularly relevant for research applications focused on non-small cell lung cancer (NSCLC). -
EGFR Inhibitor
EAI001 is a potent allosteric inhibitor of the mutant epidermal growth factor receptor (EGFR), specifically targeting the EGFRL858R/T790M variant with an IC50 of 24 nM. This compound demonstrates selective inhibition of aberrant EGFR signaling, making it valuable for investigating its role in cancer biology and therapeutic resistance. EAI001 serves as a critical tool for research aimed at understanding and developing treatments for EGFR-mutated tumors. -
EGFR/ErbB Inhibitor
EGFR/ErbB-2-IN-2 is a potent inhibitor of the epidermal growth factor receptor (EGFR) and ErbB family of receptor tyrosine kinases. It exhibits IC50 values of 0.017 μM for EGFR, 0.08 μM for ErbB-2, and 1.91 μM for ErbB-4, highlighting its selectivity and efficacy. This compound is valuable for research applications focused on cancer biology, particularly in the study of signaling pathways and mechanisms associated with EGFR and ErbB receptor activation. -
EGFR Inhibitor
Rociletinib hydrobromide is a selective inhibitor of mutant forms of the epidermal growth factor receptor (EGFR), particularly effective against the T790M mutation. It demonstrates a Ki value of 21.5 nM for the EGFRL858R/T790M variant, while maintaining a Ki of 303.3 nM for wild-type EGFR. This compound is relevant for research applications aimed at understanding and developing targeted therapies for EGFR-mutant cancers. -
EGFR Inhibitor
Tyrphostin AG 112 is a selective inhibitor of epidermal growth factor receptor (EGFR) phosphorylation. This compound has been shown to interfere with EGFR signaling pathways, resulting in the inhibition of cell proliferation and survival in various cancer cell lines. Tyrphostin AG 112 is utilized in research applications aimed at understanding EGFR-mediated processes and developing targeted therapies for EGFR-associated tumors. -
HER2/EGFR Inhibitor
Neratinib maleate is an orally available, irreversible inhibitor targeting HER2 and EGFR with IC50 values of 59 nM and 92 nM, respectively. This compound demonstrates significant anti-tumor activity and is utilized in research for its applications in cancer therapy, particularly in tumors exhibiting overexpression of HER2. Its selective inhibition profile makes it a valuable tool for studies exploring resistance mechanisms and therapeutic efficacy in targeted cancer treatment. -
EGFR-HER2 Inhibitor
Sevabertinib is a potent and reversible dual inhibitor of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2), exhibiting IC50 values below 0.5 nM for both wild-type HER2 and various mutant forms, including HER2 A775insYVMA, as well as wild-type EGFR and EGFR D770_N771insSVD. This compound demonstrates significant anticancer activity, particularly against lung cancer, making it a valuable tool for research in targeted cancer therapies and signaling pathway studies. -
EGFR/ErbB2 Inhibitor
PD 174265 is a highly selective, reversible inhibitor of the EGFR and ErbB2 tyrosine kinases, demonstrating an IC50 of 0.45 nM. This compound effectively inhibits receptor autophosphorylation and the downstream ERK signaling pathway, leading to significant antitumor activity and reduced toxicity in in vivo models. Additionally, PD 174265 facilitates the differentiation of oligodendrocyte precursor cells, promoting the expression of myelin proteins such as CNP, PLP, and MBP, and enhancing neurite branching. With no inhibitory effect on other kinases like insulin and PDGF receptors, PD 174265 is a vital tool for researching human epidermoid carcinoma treatment and myelin repair mechanisms in multiple sclerosis. -
EGFR/ERBB2 Inhibitor
HKI-357 is an irreversible dual inhibitor targeting EGFR and ERBB2, exhibiting IC50 values of 34 nM for EGFR and 33 nM for ERBB2. This compound effectively suppresses EGFR autophosphorylation at tyrosine 1068, leading to the inhibition of downstream signaling pathways, including AKT and MAPK phosphorylation. HKI-357 is valuable for research into cancer therapies that target these critical signaling pathways. -
EGFR Inhibitor
EGFR-IN-70 is a potent inhibitor of the epidermal growth factor receptor (EGFR), exhibiting IC50 values of 23.6 nM and 307.5 nM for EGFR-LR/TM/CS and EGFR-WT, respectively. This compound demonstrates significant anti-proliferative effects and effectively suppresses EGFR phosphorylation. EGFR-IN-70 is a valuable tool for cancer research, particularly in studies focusing on EGFR-related signaling pathways and therapeutic interventions. -
EGFR Kinase Inhibitor
PF-06672131 is a potent inhibitor of the epidermal growth factor receptor (EGFR) kinase, targeting the ATP-binding pocket through its alkynylated afatinib derivative structure. This small molecule probe displays reactivity to cysteine and is valuable for activity-based protein profiling studies. Its ability to effectively inhibit EGFR makes it a useful tool in cancer research, particularly in exploring therapeutic strategies for EGFR-driven malignancies. -
EGFR Tyrosine Kinase Inhibitor
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). -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
Mutant-Selective EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
(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. -
EGFR Inhibitor
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. -
Alflutinib Metabolite/EGFR Inhibitor
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. -
EGFR-TKI Inhibitor
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. -
EGFR/ErbB2 Inhibitor
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. -
EGFR Mutants Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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). -
TrxR/EGFR Inhibitor
TrxR/EGFR-IN-1 is a potent inhibitor targeting both Thioredoxin Reductase (TrxR) and Epidermal Growth Factor Receptor (EGFR). This compound demonstrates significant anti-proliferative effects against Gefitinib-sensitive and resistant lung cancer cells, facilitating apoptosis and tumor cell death. TrxR/EGFR-IN-1 promotes GPX4 protein degradation via autophagolysosomal and proteasomal pathways, leading to ferroptosis. Additionally, it induces endoplasmic reticulum stress and triggers immunogenic cell death, making it a valuable tool for studying mechanisms underlying Gefitinib-resistant lung cancer. -
ErbB-2/EGFR Inhibitor
Lapatinib tosylate is a potent inhibitor targeting the ErbB-2 and EGFR tyrosine kinase domains. With IC50 values of 10.2 nM for EGFR and 9.8 nM for ErbB-2, it effectively blocks signaling pathways associated with cell proliferation and survival. This compound is primarily utilized in cancer research and therapeutic studies, particularly for conditions driven by aberrant ErbB signaling. -
STAT3 Inhibitor
W1131 is a potent inhibitor of signal transducer and activator of transcription 3 (STAT3), which plays a critical role in oncogenic processes. By inducing ferroptosis, W1131 effectively suppresses cancer progression in various models, including gastric cancer subcutaneous xenografts, organoids, and patient-derived xenografts (PDX). Additionally, W1131 enhances chemosensitivity of cancer cells to 5-fluorouracil (5-FU), while modulating cell cycle dynamics, DNA damage response, and oxidative phosphorylation via the IL6-JAK-STAT3 and ferroptosis pathways. This compound is valuable for research into cancer biology and therapeutic resistance. -
JAK3 Inhibitor
JAK3-IN-13 is a selective and orally bioavailable inhibitor of JAK3, exhibiting IC50 values of 4728, 2039, 8, and 365 nM against NK1, JNK2, JNK3, and Tyk2, respectively. This compound demonstrates significant antiproliferative effects and induces cell cycle arrest in the G0/G1 phase. JAK3-IN-13 is particularly relevant for research applications focused on tumor biology and the modulation of immune responses. -
PIM-3 Inhibitor
M-110 is a selective, ATP-competitive inhibitor of PIM kinases, prominently targeting PIM-3 with an IC50 of 47 nM. This compound exhibits inhibitory activity against PIM-1 and PIM-2 with IC50 values around 2.5 μM. M-110 has demonstrated efficacy in curtailing the proliferation of prostate cancer cell lines, exhibiting IC50 values ranging from 0.6 to 0.9 μM. This makes M-110 a valuable tool for studying PIM kinase signaling pathways and their role in cancer biology. -
Pim-2 Inhibitor
HJ-PI01, a potent Pim-2 inhibitor, effectively induces apoptosis and autophagic cell death in cancer cells. This compound demonstrates significant anti-tumor activity in vivo, notably inhibiting tumor growth in MDA-MB-231 xenograft mouse models. HJ-PI01 serves as a valuable tool for cancer research, facilitating investigations into the therapeutic implications of Pim-2 inhibition. -
PIM Inhibitor
Uzansertib is a potent, orally active pan-PIM kinase inhibitor that operates through ATP-competitive mechanisms, exhibiting IC50 values of 0.24 nM, 30 nM, and 0.12 nM for PIM1, PIM2, and PIM3, respectively. This compound demonstrates significant anti-proliferative activity across a range of hematologic tumor cell lines, making it a valuable tool for research in cancer biology and therapeutic development. Researchers can utilize Uzansertib to explore the roles of PIM kinases in tumorigenesis and potential treatment strategies. -
Pim-1/2 Kinase Inhibitor
Pim-1/2 kinase inhibitor 1 is a selective inhibitor of Pim-1 and Pim-2 kinases, targeting their phosphorylation activity. This compound effectively disrupts the phosphorylation of key substrates, including 4E-BP1 and p27Kip1, which are crucial for cell cycle regulation and protein synthesis. Pim-1/2 kinase inhibitor 1 is primarily utilized in cancer research, particularly in studies focusing on the mechanisms underlying prostate cancer progression. -
PIM Inhibitor
AZD1897 is a potent inhibitor of PIM1, PIM2, and PIM3 kinases, demonstrating IC50 values of less than 3 nM for each target. This compound exhibits significant anticancer activity, particularly in acute myeloid leukemia (AML) cells, where it shows a synergistic effect when used in combination with Capivasertib. The mechanism of action involves the inhibition of critical cellular pathways, including mTOR and MCL1, making AZD1897 a valuable tool for cancer research. -
Pim Inhibitor
K00135 is a potent and selective inhibitor of PIM kinases, primarily targeting PIM1, PIM2, and PIM3. This compound demonstrates significant inhibition of cell survival and clonogenic growth in acute leukemia cells. Additionally, K00135 effectively reduces the phosphorylation of downstream targets of the PIM signaling pathway, making it a valuable tool for cancer research focusing on PIM kinase-related mechanisms. -
Pim/DAPK3 Inhibitor
HS56 is an ATP-competitive dual inhibitor of Pim kinases and DAPK3, demonstrating Ki values of 0.26 μM for DAPK3, 0.208 μM for Pim-3, and over 100 μM for Pim-2 and Pim-1. This compound effectively inhibits LC20 phosphorylation and smooth muscle contraction, leading to a reduction in blood pressure in spontaneously hypertensive mouse models. HS56 is suitable for research investigating the mechanisms and potential treatments for hypertension. -
Pim-1 Kinase Inhibitor
Pim-1 Kinase Inhibitor 13 is a selective inhibitor of Pim-1 kinase, exhibiting an IC50 of 4.41 μM. This compound is instrumental in the study of immunological processes and cancer biology, providing valuable insights into Pim-1's role in cell survival and proliferation. Its application in research may facilitate the development of targeted therapies for malignancies associated with aberrant Pim-1 activity. -
Pim Inhibitor
DHPCC-9 is a selective inhibitor of Pim kinase, a critical regulator of cell survival and proliferation. This compound demonstrates potent biological activity in modulating cancer cell growth and has significant implications for cancer research, particularly in the investigation of therapeutic strategies targeting the Pim signaling pathway. Researchers can utilize DHPCC-9 to explore its effects on cellular responses and potential applications in developing anti-cancer therapies. -
Pim Inhibitor
R8-T198wt is a cell-permeable peptide that functions as a Pim-1 kinase inhibitor. By targeting the carboxyl-terminal region of p27Kip1, it exhibits significant anti-tumor activity. This reagent is ideal for research applications involving cancer biology and cellular signaling pathways associated with cell cycle regulation and apoptosis. -
Pan-PIM Inhibitor
GDC-0570 is a potent and selective pan-PIM inhibitor designed for oral administration. It exhibits pronounced antitumor activity and has shown synergistic effects when combined with Sotorasib in models of acquired KRAS-resistant non-small cell lung cancer (NSCLC). This compound serves as a valuable tool for investigating the role of PIM kinases in cancer biology and therapeutic resistance. -
PIM-1 Inhibitor
PIM1-IN-7 is a potent inhibitor of the PIM-1 kinase, exhibiting an IC50 of 0.67 μM. This compound demonstrates significant cytotoxicity against HCT-116 and MCF-7 cancer cell lines, with IC50 values of 42.9 μM and 7.68 μM, respectively. Its ability to selectively inhibit PIM-1 makes it a valuable tool for investigating the role of this kinase in cancer biology and for exploring potential therapeutic strategies. -
Pim-1 Inhibitor
Pim-1 kinase inhibitor 5 is a selective inhibitor of Pim-1 kinase, exhibiting an IC50 value of 0.61 μM. This compound demonstrates significant cytotoxicity across various cancer cell lines, including HepG2, MCF-7, PC3, and HCT-116, with IC50 values ranging from 6.95 to 20.19 μM. It serves as a valuable tool for researching the modulation of Pim-1 in cancer biology and therapeutic applications. -
PIM Inhibitor
FD1024 is a potent PIM inhibitor with IC50 values of 1.96 nM, 38.9 nM, and 4.17 nM for PIM1, PIM2, and PIM3, respectively. This compound exhibits strong antiproliferative activity against various acute myeloid leukemia (AML) cell lines, showing effective concentrations of 0.16 μM, 0.12 μM, 1.05 μM, and 1.39 μM for EOL-1, MV-4-11, KG-1, and MOLM-16 cells. Additionally, FD1024 demonstrates significant antitumor efficacy in in vivo mouse models, making it a valuable tool for research into AML therapeutic strategies.
