Protein Tyrosine Kinases

Items 1301-1350 of 1870

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  1. VEGFR2 Inhibitor

    VEGFR-2-IN-19 is a potent inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR2). This compound has been shown to induce apoptosis in cancer cells and elevate intracellular levels of reactive oxygen species. VEGFR-2-IN-19 is primarily utilized in cancer research, offering potential therapeutic insights into tumor progression and vascularization.
  2. FLT3 Inhibitor

    JH-IX-179 is a potent FLT3 inhibitor with an IC50 of 4 nM for FLT3-ITD and 10 nM for FLT3-D835Y variants. This compound effectively induces cell cycle arrest in the G1 phase and promotes apoptosis in cells expressing the FLT3-ITD mutation. JH-IX-179 is primarily utilized in research focused on acute myeloid leukemia (AML), providing valuable insights into therapeutic strategies targeting FLT3 signaling pathways.
  3. CSF-1R Inhibitor

    CSF1R-IN-22 is a selective inhibitor of the colony-stimulating factor 1 receptor (CSF-1R) with an IC50 value of less than 6 nM. This compound enhances CXCL9 secretion from M2 macrophages and promotes CD8+ T cell infiltration, thereby amplifying anti-tumor immune responses, particularly in combination with anti-PD-1 therapies. CSF1R-IN-22 effectively reprograms M2-like tumor-associated macrophages (TAMs) to the M1 phenotype, reshaping the tumor microenvironment by increasing CD8+ T cell recruitment and decreasing immunosuppressive regulatory T cells and myeloid-derived suppressor cells (MDSCs).
  4. FLT3/HDAC Inhibitor

    HDAC-IN-63 is a dual inhibitor targeting both FLT3 and HDAC, with IC50 values of 0.844 nM for FLT3 and 30.0 nM for HDAC1. It demonstrates potent inhibition of MV4-11 cell proliferation, with an IC50 of 92 nM, and effectively induces apoptosis while arresting the cell cycle in MV4-11 cells. This compound serves as a valuable research tool for the study of acute myeloid leukemia (AML) and the exploration of novel therapeutic strategies.
  5. 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.
  6. VEGFR-2 Inhibitor

    VEGFR-2-IN-13 is a potent inhibitor of the vascular endothelial growth factor receptor-2 (VEGFR-2), demonstrating an IC50 value of 3.4 nM. This compound effectively disrupts the cell cycle in HepG2 cells by inducing G2/M phase arrest and triggering apoptosis. VEGFR-2-IN-13 is valuable for research applications focusing on angiogenesis, cancer development, and therapeutic interventions targeting tumor growth.
  7. VEGFR-2 Inhibitor

    VEGFR-2-IN-28 is a selective inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR-2) with an IC50 value of 0.83 µM. This compound has been shown to induce apoptosis in cancer cells, highlighting its potential as an anticancer agent. VEGFR-2-IN-28 is suitable for research applications focused on tumor vascularization and the mechanisms of cancer cell survival signaling.
  8. FLT3 Inhibitor

    FLT3-IN-31 is a potent inhibitor of FLT3, exhibiting IC50 values of 0.16 nM for the wild-type FLT3 receptor and 2.4 nM for the FLT3-D835Y mutant. It demonstrates significant antiproliferative activity by decreasing the protein expression of phosphorylated FLT3, STAT5, and ERK. Additionally, FLT3-IN-31 induces apoptosis and triggers cell cycle arrest at the G1 phase, making it a valuable tool for research in targeted cancer therapies and leukemia treatment.
  9. FLT3/HDAC Inhibitor

    FLT3/HDAC-IN-3 is a dual inhibitor targeting FLT3 and HDAC, with a potent inhibitory effect on FLT3 (IC50 = 14 nM) and HDAC isoforms, including HDAC1 (IC50 = 27 nM) and HDAC6 (IC50 = 20 nM). This compound demonstrates selective inhibition, exhibiting reduced activity against HDAC8 and no activity toward HDAC4. FLT3/HDAC-IN-3 has shown anti-proliferative effects across various hematological malignancy cell lines and demonstrates efficacy in the Jeko-1 xenograft model without significant toxicity. It is suitable for research focused on hematological malignancies and the role of dual inhibition in therapeutic strategies.
  10. SRC Inhibitor

    SI-2 is a selective inhibitor of steroid receptor coactivator-3 (SRC-3), effectively reducing both its transcriptional activity and protein levels in cells. This compound exhibits significant cytotoxicity against cancer cells and inhibits the migration of MDA-MB-468 breast cancer cells, promoting apoptosis in these cells. In vivo studies demonstrate that SI-2 suppresses tumor growth in mouse models while showing minimal toxicity to the heart and other vital organs at a dosage of 20 mg/kg.
  11. PROTAC c-Met Degrader

    PROTAC c-Met Degrader-4 is a potent orally active PROTAC designed to target c-MET for degradation. It exhibits remarkable intracellular degradation potency with a DC50 value of less than 0.5 nM and effectively induces cell cycle arrest and apoptosis while inhibiting cell invasion and migration. This compound is particularly useful in cancer research, demonstrating the ability to suppress proliferation and inhibit the growth of various cancers, including non-small cell lung cancer and gastric cancer. In vivo studies also highlight its effectiveness in reducing tumor growth in Hs746T xenograft models.
  12. FLT3/JAK2 Inhibitor

    JAK2/FLT3-IN-3 is a potent dual inhibitor of FLT3 and JAK2, exhibiting IC50 values of 2.01 nM for JAK2, 0.51 nM for FLT3, and 104.40 nM for JAK3. This compound induces apoptosis in cancer cells and demonstrates significant antitumor activity. Its ability to inhibit both FLT3 and JAK2 pathways makes it a valuable tool for research related to hematological malignancies and targeted cancer therapies.
  13. ALK Inhibitor

    KF-20444 is a selective ALK inhibitor that effectively penetrates the blood-brain barrier. It demonstrates potent activity against ALK fusion proteins such as EML4-ALK and various ALK resistance mutations, including L1196M, G1202R, and F1174L. By inhibiting ALK phosphorylation in ALK-driven cancer cell lines, KF-20444 suppresses cell proliferation and promotes apoptosis. This compound shows significant anti-tumor efficacy in mouse models of ALK-positive non-small cell lung cancer (NSCLC) and neuroblastoma, making it a valuable tool for research on ALK-driven malignancies.
  14. 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.
  15. 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.
  16. 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.
  17. 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.
  18. 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.
  19. 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.
  20. 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.
  21. 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.
  22. 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.
  23. 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.
  24. 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.
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. 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.
  32. Anti-Inflammatory Agent

    2,4′-Dihydroxybenzophenone acts as an anti-inflammatory agent by targeting the hydrophobic pocket of MD2, effectively inhibiting the dimerization of TLR4. This compound demonstrates significant biological activity by suppressing LPS-induced mitochondrial reactive oxygen species (mtROS) production and attenuating the inflammatory response through downregulation of pro-inflammatory mediators, including MyD88, p-IRAK4, and NF-κB. Additionally, 2,4′-Dihydroxybenzophenone serves as an effective UV absorber, enhancing its utility in research on oxidative stress and inflammation.
  33. IRAK4 PROTAC Degrader

    PROTAC IRAK4 degrader-13 is a selective IRAK4-directed PROTAC degrader that effectively targets IRAK4 with DC50 values of 0.86 nM and 1.1 nM in monocytes and lymphocytes, respectively. This compound significantly activates TIR signaling and reduces the expression of proinflammatory cytokines in an Imiquimod-induced psoriasis mouse model. PROTAC IRAK4 degrader-13 is applicable in research focused on TLR- and IL-1R-driven inflammatory diseases, including hidradenitis suppurativa and atopic dermatitis.
  34. 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.
  35. IRAK PROTAC Degradant

    APH02174 is a highly selective IRAK4 PROTAC degrader that exhibits an impressive DC50 value of 4.01 nM in THP-1 cells. By effectively inhibiting the release of IL-6, APH02174 serves to block inflammatory signaling pathways. This compound is valuable for research into various inflammatory conditions, including psoriasis vulgaris and rheumatoid arthritis.
  36. c-Kit Receptor Modulator

    c-Kit Receptor modulator-1 is a selective modulator of the c-Kit receptor, primarily involved in cell signaling pathways associated with hematopoiesis and mast cell function. This compound exhibits potent activity against malignancies such as canine mastocytoma, human gastrointestinal stromal tumors, and small cell lung cancer. It is a valuable tool for research focused on tumor biology and therapeutic interventions targeting c-Kit signaling pathways.
  37. 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.
  38. 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.
  39. 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.
  40. 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.
  41. 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.
  42. 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.
  43. 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.
  44. 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.
  45. 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.
  46. 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.
  47. 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.
  48. 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.
  49. 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.
  50. 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.

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