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Catalog No.
Product Name
Application
Product Information
Citations
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FGFR2 Kinase Inhibitor
Picrasidine Q is a FGFR2 kinase inhibitor derived from the alkaloid components of Angelica keiskei. It exhibits significant anti-cancer properties by inducing apoptosis and causing G1 phase cell cycle arrest in human esophageal cancer cell lines. This compound is valuable for research focused on cancer biology and the molecular mechanisms underlying cell transformation and proliferation. -
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. -
VEGFR-2/β-tubulin Inhibitor
VEGFR-2-IN-22 is a dual inhibitor targeting VEGFR-2 and β-tubulin polymerization, demonstrating an IC50 of 19.82 nM against VEGFR-2. This compound promotes apoptosis, making it a valuable tool for studying angiogenesis and cancer biology. Its mechanism of action provides insights into vascular endothelial growth factor pathways and their role in tumor progression. -
FLT3 Inhibitor
Tuspetinib dihydrochloride is a selective FLT3 inhibitor that demonstrates potent inhibitory activity with IC50 values of 1.1 nM for FLT3 WT, 1.8 nM for FLT3 ITD, and 1.0 nM for FLT3 D835Y kinases. As a reversible type I inhibitor, it effectively modulates downstream signaling pathways, including p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib dihydrochloride is utilized in research for its ability to inhibit proliferation and induce apoptosis in leukemic cells, making it significant for studies on hematological malignancies. -
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. -
FLT3/MNK2 Inhibitor
K783-0308 is a potent and selective dual inhibitor of FLT3 and MNK2, demonstrating IC50 values of 680 nM and 406 nM, respectively. This compound effectively inhibits the growth of acute myeloid leukemia (AML) cell lines, MOLM-13 and MV-4-11, with IC50 values of 10.5 µM and 10.4 µM. Additionally, K783-0308 promotes apoptosis and induces cell cycle arrest in the G0/G1 phase, making it a valuable tool for research into AML and related pathways. -
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. -
FLT3-ITD Inhibitor
FLT3-ITD-IN-3 is a potent inhibitor of FLT3-ITD (FLT3 internal tandem duplication), primarily targeting the FLT3 signaling pathway. This compound effectively disrupts FLT3 signal transduction, leading to G0/G1 cell cycle arrest and the induction of apoptosis in malignant cells. FLT3-ITD-IN-3 is valuable for research applications focused on acute myeloid leukemia (AML) and related hematological disorders. -
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. -
PARP1/c-Met Inhibitor
PARP1/c-Met-IN-1 is a selective dual inhibitor targeting PARP1 and c-Met, demonstrating IC50 values of 3.3 nM and 32.2 nM, respectively. This compound effectively induces apoptosis and causes cell cycle arrest in the G2/M phase in MDA-MB-231 cells. Additionally, PARP1/c-Met-IN-1 has shown significant antitumor activity in murine models, making it a valuable tool for cancer research and therapeutic development. -
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. -
FLT3 Inhibitor
FLT3-IN-33 is a potent FLT3 inhibitor with an IC50 value of 7.82 nM, demonstrating significant anti-cancer activities, particularly against acute myeloid leukemia (AML) cell lines such as MV4-11 and MOLM-13. This compound effectively induces apoptosis in cancer cells and inhibits the phosphorylation of FLT3 signaling pathways. FLT3-IN-33 is suitable for research applications targeting AML and other malignancies, providing valuable insights into therapeutic strategies and cellular responses. -
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/VEGFR2 Inhibitor
EGFR/VEGFR2-IN-3 is a selective inhibitor of the epidermal growth factor receptor (EGFR) and vascular endothelial growth factor receptor 2 (VEGFR-2), demonstrating IC50 values of 0.129 µM and 0.142 µM, respectively. This compound also exhibits activity against cyclooxygenase-2 (COX-2) with an IC50 of 3.428 µM. EGFR/VEGFR2-IN-3 has been shown to induce cytotoxic effects, promoting apoptosis and causing cell cycle arrest at the G2/M phase. Its dual inhibition profile makes it a valuable tool for research in cancer biology and therapeutic development. -
IRAK4 Inhibitor
BMS-986126 is a potent and selective inhibitor of IRAK4, with an IC50 value of 5.3 nM. It effectively disrupts MyD88-dependent signaling pathways, thereby attenuating inflammatory responses associated with autoimmune conditions. In preclinical studies, BMS-986126 has demonstrated significant efficacy in murine models of lupus, including MRL/lpr and NZB/NZW strains. This compound is valuable for research applications related to systemic lupus erythematosus (SLE) and other autoimmune diseases. -
C-Kit Inhibitor
c-Kit-IN-12 is a potent inhibitor of the c-Kit receptor with an IC50 value of less than 10 nM in various KIT mutant cell lines, including BAF3 KIT EX11 DEL, EX11 DEL/D816H, EX11 DEL/T670I, and EX11 DEL/V654A. This compound is valuable for investigating c-Kit-related pathologies, particularly in cancer research. Its specificity and efficacy make it a useful tool for elucidating the role of c-Kit in oncogenic processes and for exploring potential therapeutic strategies. -
C-Kit Inhibitor
(S)-c-Kit-IN-12 is a potent c-Kit inhibitor, exhibiting an IC50 value of less than 10 nM across four different KIT mutant cell models, including BAF3 KIT EX11 DEL, EX11 DEL/D816H, EX11 DEL/T670I, and EX11 DEL/V654A. This compound is suitable for investigating c-Kit-related diseases, particularly in cancer research applications, where dysregulation of c-Kit signaling is implicated. -
CSF-1R Inhibitor
Sotuletinib hydrochloride is a potent and selective inhibitor of the CSF-1R (c-Fms) with an IC50 value of 1 nM, demonstrating over 1,000-fold selectivity against related receptor tyrosine kinases. This orally bioavailable and brain-penetrant compound is utilized in research focused on microglia depletion, tumor biology, and central nervous system-related diseases, making it a valuable tool for advancing understanding in these areas. -
CSF1R Inhibitor
SYHA1813 is an inhibitor of the colony-stimulating factor 1 receptor (CSF1R) that demonstrates potent antitumor activity, particularly in glioblastoma (GBM). By targeting CSF1R, SYHA1813 modulates the tumor microenvironment and affects immune cell infiltration, making it a valuable tool for studying tumor progression and therapeutic resistance. This compound can be utilized in preclinical research to explore its efficacy in cancer treatment strategies. -
CSF1R Inhibitor
Enrupatinib is a selective inhibitor of colony-stimulating factor 1 receptor (CSF1R) with potent oral bioavailability and central nervous system (CNS) penetration. It effectively inhibits macrophage proliferation and osteoclast differentiation in vitro, thereby mitigating neuroinflammation and preserving neuronal integrity in Alzheimer's disease models. Enrupatinib has demonstrated the ability to reduce disease-associated microglia gene expression and enhance cognitive function in 5xFAD and J20 mouse models. Additionally, it attenuates tumor-associated macrophage infiltration and improves the antitumor efficacy of anti-PD-1 antibodies in preclinical models of colorectal and breast cancer, making it a valuable tool for research in these areas. -
CSF1R Inhibitor
AZ683 is a selective inhibitor of the colony stimulating factor 1 receptor (CSF1R), with a high binding affinity (Ki=8 nM; IC50=6 nM). This compound demonstrates good oral bioavailability, making it suitable for in vivo studies. Additionally, [11C]AZ683 serves as a positron emission tomography (PET) radiotracer for visualizing CSF1R activity, enabling insights into its role in various biological processes and diseases. This compound is valuable for research applications focused on immune modulation and tumor microenvironment studies. -
CSF1R Inhibitor
CSF1R-IN-12 is a potent inhibitor of colony stimulating factor 1 receptor (CSF1R), which plays a crucial role in regulating bone marrow progenitor cells, monocytes, macrophages, and giant cells. By targeting CSF1R, this compound exhibits significant potential for cancer research, particularly in studies focused on the modulation of macrophage activity and tumor microenvironment interaction. CSF1R-IN-12 can aid in elucidating the role of CSF1R in various malignancies and in the development of novel therapeutic strategies. -
CSF1R Inhibitor
CSF1R-IN-24 is an orally active inhibitor of the colony-stimulating factor 1 receptor (CSF1R). This compound significantly reduces the survival of human induced pluripotent stem cell-derived microglia (hiPSC-MG), making it a valuable tool for studying microglial biology and potential therapeutic applications in neuroinflammatory conditions. Researchers can utilize CSF1R-IN-24 to investigate the role of microglia in various disease models and to explore new treatment strategies targeting the CSF1R pathway. -
CSF-1R Inhibitor
CSF1R-IN-3 is a potent and orally bioavailable inhibitor of the colony-stimulating factor 1 receptor (CSF-1R), with an IC50 of 2.1 nM. This compound exhibits significant antiproliferative activity against colorectal cancer cells by inhibiting the progression of the disease through the suppression of macrophage migration. Additionally, CSF1R-IN-3 facilitates the reprogramming of M2-like macrophages into the M1 phenotype, thereby enhancing antitumor immunity. This compound serves as a valuable tool for research in cancer immunology and macrophage biology. -
CSF1R/Mer/Axl Inhibitor
Adrixetinib is a potent triple inhibitor targeting CSF1R, Mer, and Axl, with Kd values of 8.7 nM, 0.8 nM, and 0.3 nM respectively. This compound serves as an effective immune modulator by remodeling the tumor microenvironment, enhancing the presence of M1 macrophages and CD8⁺ T cells while reducing M2 macrophages and myeloid-derived suppressor cells (MDSCs). Additionally, Adrixetinib increases the expression of MHC class I and E-cadherin in tumor cells, demonstrating significant antitumor efficacy in syngeneic mouse models. It is relevant for research involving breast cancer, renal adenocarcinoma, colon carcinoma, and melanoma. -
CSF1R Inhibitor
BPR1R024 mesylate is a selective inhibitor of the colony-stimulating factor-1 receptor (CSF1R), demonstrating potent inhibitory activity with an IC50 value of 0.53 nM. This compound is orally active and serves as a valuable tool for research in immuno-oncology, facilitating the exploration of CSF1R's role in tumor microenvironments and immune system modulation. BPR1R024 mesylate's targeted action enables detailed studies of its effects on macrophage biology and associated therapeutic strategies. -
PI3Kδ/CSF1R Inhibitor
JMC14 is a selective PI3Kδ and CSF1R inhibitor, exhibiting IC50 values of 12 nM and 143 nM, respectively. This compound preferentially disrupts PI3Kδ-mediated signaling within cells, demonstrating significant antitumor activity against B-cell lymphomas and triple-negative breast cancer (TNBC) in both in vitro and in vivo models. JMC14 is an important tool for research into antitumor immunity and the mechanisms of cancer progression. -
CSF1-R Inhibitor
Sotuletinib dihydrochloride is a highly selective and potent inhibitor of the colony-stimulating factor 1 receptor (CSF1-R or c-Fms), exhibiting an IC50 of 1 nM and over 1,000-fold selectivity against closely related receptor tyrosine kinases. This compound is effective for the depletion of microglia and is valuable in research applications related to tumors and central nervous system (CNS) disorders. Its oral bioavailability and ability to penetrate the blood-brain barrier enhance its utility in neuropharmacological studies. -
Axl/Mer/CSF1R Inhibitor
Axl/Mer/CSF1R-IN-2 is a selective inhibitor targeting Axl, Mer, and CSF1R receptors. This compound demonstrates potent inhibition of these receptor kinases, which are implicated in various cancer types and immune response regulation. It is suitable for research applications focusing on tumor microenvironment modulation, immune checkpoint interactions, and potential therapeutic strategies in oncological studies. -
CSF1R Inhibitor
IACS-9439 is a potent and selective inhibitor of the colony-stimulating factor 1 receptor (CSF1R) with a Ki value of 1 nM. This orally active compound demonstrates significant potential in cancer research, particularly for the treatment of advanced solid tumors. It enables investigation into the role of CSF1R in tumor microenvironments and immune modulation. -
CSF1R Inhibitor
CSF1R-IN-5 is a potent inhibitor of the colony-stimulating factor 1 receptor (CSF1R), which plays a critical role in the survival and differentiation of macrophages. By targeting the CSF-1/CSF-1R signaling pathway, CSF1R-IN-5 modulates the interaction between tumor-associated macrophages (TAMs) and glioma cells, influencing the exchange of inflammatory mediators. This compound is useful for research applications in cancer biology, particularly in studies investigating the tumor microenvironment and macrophage function in oncogenesis. -
CSF-1R Inhibitor
CSF1R-IN-7 is a selective inhibitor of Colony Stimulating Factor 1 Receptor (CSF-1R). This compound demonstrates potential in modulating microglial activation, making it a valuable tool for research in neuroinflammatory conditions such as Alzheimer’s disease. It is particularly useful for studying the role of CSF-1R in the pathology and progression of neurodegenerative disorders. -
CSF-1R Inhibitor
CSF1R-IN-9 is a selective inhibitor of the colony-stimulating factor 1 receptor (CSF-1R), demonstrating an IC50 of 0.028 μM. This compound effectively disrupts CSF-1R signaling, making it valuable for research on macrophage biology and inflammation. CSF1R-IN-9 can be utilized in investigating therapeutic strategies for conditions such as cancer and autoimmune diseases. -
CSF1R Inhibitor
CSF1R-IN-14 is a potent inhibitor of the colony stimulating factor 1 receptor (CSF1R). As an isoindolinone derivative, it effectively modulates the activity of CSF-1, a key growth factor regulating the development and function of monocytes and macrophages. This compound holds potential for advancing research in cancer biology and studying immune responses associated with tumor progression. -
CSF1R Inhibitor
CSF1R-IN-23 is a selective inhibitor of colony-stimulating factor-1 receptor (CSF1R) with an IC50 of 36.1 nM. This compound demonstrates significant neuroinflammatory activity in mouse models, making it a valuable tool for studying neuroinflammation and related pathways. Additionally, CSF1R-IN-23 is permeable to the blood-brain barrier (BBB), facilitating its use in neurological research applications. -
CSF1R Inhibitor
CSF1R-IN-4 is a selective inhibitor of the colony-stimulating factor 1 receptor (CSF1R). This compound plays a critical role in modulating macrophage survival and differentiation by targeting the CSF-1/CSF-1R signaling pathway. CSF1R-IN-4 has been shown to influence the interaction between tumor-associated macrophages (TAMs) and glioma cells, making it a valuable tool for cancer research. Its potential applications include studying the tumor microenvironment and the immune response in various malignancies. -
CSF1R Inhibitor
CSF1R-IN-25 is a selective inhibitor of the Colony Stimulating Factor 1 Receptor (CSF1R). This compound demonstrates significant potential in modulating biological processes related to cancer, inflammation, and neurodegeneration. It serves as a valuable tool for researchers investigating the therapeutic implications of CSF1R inhibition in these areas. -
CSF1R Inhibitor
CSF1R-IN-19 is a potent inhibitor of the colony-stimulating factor 1 receptor (CSF1R). It modulates the interaction between tumor-associated macrophages and glioma cells, influencing the exchange of inflammatory factors. This compound is significant for cancer research, particularly in understanding the tumor microenvironment and exploring therapeutic strategies targeting CSF1R. -
Axl/Mer/CSF1R Inhibitor
Axl/Mer/CSF1R-IN-1 is an inhibitor of Axl/Mer receptor tyrosine kinases and CSF1R, demonstrating a binding affinity with Kds of less than 0.1 μM. This compound is valuable for research focused on the modulation of signaling pathways related to cancer, inflammation, and immune response. Its ability to precisely inhibit these targets makes it a useful tool in studies investigating the roles of Axl, Mer, and CSF1R in various biological processes. -
CSF-1R Inhibitor
CSF1R-IN-8 is a potent inhibitor of colony-stimulating factor 1 receptor (CSF-1R) with an IC50 of 0.012 μM. This compound exhibits significant biological activity in modulating CSF-1R signaling pathways, which are crucial for monocyte and macrophage differentiation and function. CSF1R-IN-8 is applicable in research focusing on immunology, cancer therapy, and the study of tumor microenvironments. -
CSF1R Inhibitor
CSF1R-IN-13 is a potent inhibitor of the colony stimulating factor 1 receptor (CSF1R). As a crucial growth factor, CSF-1 modulates the development of bone marrow progenitor cells, monocytes, and macrophages, influencing immune response and cancer progression. This compound serves as a valuable research tool for investigating CSF1R's role in cancer therapies and related disease mechanisms. -
CSF-1R Inhibitor
CSF1R-IN-10 is a potent inhibitor of the colony-stimulating factor 1 receptor (CSF-1R) with an IC50 of 0.005 μM. This compound effectively disrupts CSF-1R signaling, which is crucial for the regulation of macrophage proliferation and differentiation. CSF1R-IN-10 is valuable for research applications focusing on inflammatory diseases, cancer, and the immune response, where modulation of macrophage activity is of interest. -
CSF-1R Inhibitor
Edicotinib hydrochloride is a selective inhibitor of the colony-stimulating factor-1 receptor (CSF-1R), demonstrating an IC50 of 3.2 nM. This compound is brain penetrant and orally bioavailable, showing minimal off-target effects on KIT and FLT3 with IC50 values of 20 nM and 190 nM, respectively. Edicotinib hydrochloride effectively limits microglial expansion, attenuating neurodegeneration in preclinical models. Its unique profile offers potential applications in research related to Alzheimer's disease and rheumatoid arthritis. -
CSF1R Inhibitor
CSF1R-IN-21 is a potent inhibitor of the colony-stimulating factor 1 receptor (CSF1R) with an IC50 value of 31 nM. This compound effectively inhibits CSF1R auto-phosphorylation, making it a valuable tool for investigating the role of CSF1R in neurodegenerative diseases. CSF1R-IN-21 can be utilized in research studies aimed at understanding the molecular mechanisms underlying these conditions and exploring potential therapeutic interventions. -
CSF1R Inhibitor
CSF1R-IN-6 is a potent inhibitor of the colony-stimulating factor 1 receptor (CSF1R), which plays a critical role in regulating macrophage survival and differentiation through the CSF-1/CSF1R signaling pathway. This compound modulates the exchange of inflammatory mediators between tumor-associated macrophages (TAMs) and glioma cells, contributing to the understanding of tumor microenvironment interactions. CSF1R-IN-6 is a valuable tool for cancer research, particularly in elucidating the mechanisms underlying tumor progression and immune evasion. -
CSF-1R Inhibitor
CSF1R-IN-20 is a potent inhibitor of the colony stimulating factor 1 receptor (CSF-1R), exhibiting an IC50 value of 467 nM. This compound effectively inhibits CSF-1R auto-phosphorylation, thereby interfering with downstream signaling pathways. It is primarily utilized in research applications focused on understanding macrophage biology and associated diseases, including cancer and inflammatory disorders.
