Protein Tyrosine Kinases

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  1. Multikinase Inhibitor

    Multi-kinase-IN-6 is a potent multikinase inhibitor targeting TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. It demonstrates significant antiproliferative effects in cancer cell lines, with IC50 values of 3.36 μM for MCF7, 1.40 μM for HCT116, and 3.49 μM for EKVX. Furthermore, Multi-kinase-IN-6 induces cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells while promoting apoptosis, making it a valuable tool for cancer research and therapeutic studies.
  2. FGFR/HDAC Inhibitor

    HDAC-IN-50 is a potent dual inhibitor targeting FGFR and HDAC with IC50 values of 0.18 nM for FGFR1, 1.2 nM for FGFR2, 0.46 nM for FGFR3, 1.4 nM for FGFR4, and varying inhibitory effects on HDAC isoforms such as HDAC1 (1.3 nM), HDAC2 (1.6 nM), HDAC6 (2.6 nM), and HDAC8 (13 nM). This compound effectively induces apoptosis and causes cell cycle arrest at the G0/G1 phase. Additionally, HDAC-IN-50 decreases the expression of phosphorylated forms of FGFR1, ERK, and STAT3, indicating its potential applications in cancer research and therapy.
  3. VEGFR-2 Inhibitor

    VEGFR-2-IN-52 is a potent inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2), demonstrating an IC50 of 191.1 nM. This compound effectively downregulates the expression of phosphorylated VEGFR-2, MMP9, and key signaling proteins p-ERK1/2 and p-MEK1. In addition to its cytotoxic effects, VEGFR-2-IN-52 induces apoptosis and promotes cell cycle arrest in the G0/G1 phase. Furthermore, it enhances reactive oxygen species (ROS) levels, making it valuable for research in cancer therapeutics and angiogenesis studies.
  4. 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.
  5. VEGFR/PARP Inhibitor

    VEGFR/PARP-IN-1 is a dual inhibitor targeting Vascular Endothelial Growth Factor Receptor (VEGFR) and Poly(ADP-ribose) Polymerase (PARP), with IC50 values of 191 nM and 60.9 nM, respectively. This compound inhibits DNA damage repair mechanisms, induces apoptosis, and causes G2/M phase cell cycle arrest. It demonstrates significant antiproliferative activity against BRCA wild-type breast cancer cell lines, specifically MDA-MB-231 and MCF-7, with IC50 values of 4.1 μM and 3.5 μM, respectively. VEGFR/PARP-IN-1 is an effective antitumor and anti-metastatic agent, making it valuable for cancer research applications.
  6. Pan-Trk Inhibitor

    Pan-Trk-IN-3 is a potent pan-Trk inhibitor that effectively targets TrkA, TrkB, and TrkC, along with various drug-resistant mutants, exhibiting IC50 values as low as 2 nM. This compound demonstrates significant antitumor activity and induces apoptosis in cancer cells. Pan-Trk-IN-3 is suitable for research applications focusing on cancer biology and therapeutic development aimed at overcoming Trk-related resistance mechanisms.
  7. 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.
  8. 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.
  9. VEGFR-2/HDAC Dual Inhibitor

    VEGFR2/HDAC1-IN-1 is a potent dual inhibitor of VEGFR-2 and HDAC, demonstrating IC50 values of 57.83 nM and 9.82 nM, respectively. This compound effectively arrests the cell cycle at the S and G2 phases, leading to apoptosis in HeLa cells. Additionally, VEGFR2/HDAC1-IN-1 exhibits significant anti-angiogenic properties, making it a valuable tool for research in cancer biology and targeted therapies.
  10. 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.
  11. ALK/EGFR Inhibitor

    ALK/EGFR-IN-1-d5 is a deuterated dual-target inhibitor that specifically targets ALK and EGFR, exhibiting IC50 values of 1.08 nM for EGFR and 2.395 nM for ALK. This compound effectively inhibits phosphorylated proteins within the EGFR, ALK, and BRK signaling pathways, disrupting the cell cycle and subsequently promoting apoptosis through a decrease in mitochondrial membrane potential. Furthermore, ALK/EGFR-IN-1-d5 shows significant anti-tumor activity in preclinical animal models, indicating its potential for advancing research in cancer therapeutics.
  12. ALK Inhibitor

    ALK-IN-22 is a potent inhibitor of Anaplastic Lymphoma Kinase (ALK), demonstrating IC50 values of 2.3 nM, 3.7 nM, and 2.9 nM against ALK, ALKL1196M, and ALKG1202R, respectively. This compound effectively down-regulates the phosphorylation of ALK and its downstream signaling proteins, thereby inducing apoptosis in tumor cells. ALK-IN-22 is suitable for various research applications, particularly in the study of tumors associated with ALK dysregulation.
  13. IRAK4 Inhibitor

    IRAK4-IN-27 is a selective inhibitor of IRAK4, exhibiting an IC50 of 8.7 nM. This compound effectively inhibits cell growth and induces apoptosis in MYD88 L265P diffuse large B-cell lymphoma (DLBCL) cell lines. IRAK4-IN-27 is an important tool for studying the mechanisms underlying DLBCL and developing potential therapeutic strategies.
  14. JAK2/Bcr-Abl/FLT3 Inhibitor

    LS-104 is a non-ATP-competitive inhibitor targeting JAK2, Bcr-Abl, and FLT3. It effectively induces apoptosis in JAK2V617F-positive cells while inhibiting JAK2 autophosphorylation and downstream signaling pathways. Additionally, LS-104 demonstrates significant cytotoxic effects and inhibits the proliferation of FLT3-expressing leukemic cells. This hydroxystyryl-acrylonitrile compound holds potential for research into myeloproliferative disorders and refractory or relapsed hematologic malignancies.
  15. TrkB Inhibitor

    PC-046 is a potent multitarget inhibitor of tyrosine receptor kinase B (TrkB), IRAK-4, and Pim-1, with IC50 values of 13.4 μM, 15.4 μM, and 19.1 μM, respectively. This compound demonstrates significant cytotoxicity against BxPC3 pancreatic cancer cells, with an IC50 range of 7.5-130 nM. PC-046 effectively induces apoptosis and disrupts the cell cycle at the G2/M phase in these cells. Additionally, it showcases promising antitumor efficacy and favorable pharmacokinetic properties in murine models, making it a valuable tool for cancer research.
  16. 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.
  17. VEGFR Inhibitor

    VEGFR-IN-3 is a selective VEGFR inhibitor that demonstrates significant antiproliferative activity against OVCAR-4 and MDA-MB-468 cancer cell lines, with IC50 values of 0.29 μM and 0.35 μM, respectively. This compound is valuable for research applications focused on cancer biology, particularly in studies investigating angiogenesis and tumor growth modulation. Its efficacy makes it a suitable candidate for exploring therapeutic strategies targeting vascular endothelial growth factor receptor pathways.
  18. 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.
  19. IGFR Inhibitor

    Cis-NVP-ADW742 is a selective inhibitor of the insulin-like growth factor 1 receptor (IGF-1R), exhibiting a potent inhibitory effect with an IC50 of 0.17 μM. This compound also demonstrates a moderate inhibition of the insulin receptor (InsR) with an IC50 of 2.8 μM. Cis-NVP-ADW742 induces significant antiproliferative and pro-apoptotic effects in tumor cells, making it a valuable tool for cancer research and the study of signaling pathways involved in cell growth and survival.
  20. TRK Inhibitor

    IHMT-TRK-284 is a potent, orally active inhibitor targeting TRK kinases, exhibiting IC50 values of 10.5 nM, 0.7 nM, and 2.6 nM against TRKA, TRKB, and TRKC, respectively. This compound demonstrates a favorable selectivity profile within the kinome and shows promising in vivo efficacy in antitumor models. IHMT-TRK-284 is valuable for studies investigating the role of TRK signaling in various cancers and for the development of targeted therapeutic strategies.
  21. PI3K/VEGFR2 Inhibitor

    PI3K/VEGFR2-IN-1 is a highly effective dual inhibitor of PI3K and VEGFR2, exhibiting IC50 values of 2.21 μM and 68 μM, respectively. This compound has been shown to induce apoptosis in various cancer cell lines. It is suitable for research applications focused on cancer biology and therapy development targeting the PI3K/VEGFR2 signaling pathways.
  22. c-Met Inhibitor

    c-Met-IN-9 is a potent c-Met kinase inhibitor with an IC50 value of 12 nM. This 4-phenoxypyridine derivative effectively induces apoptosis in cancer cells and exhibits significant antitumor activity. It is suitable for research applications focused on cancer biology and therapeutic development targeting the c-Met signaling pathway.
  23. IGF-1R Inhibitor

    KW-2450 free base is a potent inhibitor of IGF-1 receptor (IGF-1R) and acts on multiple kinases including Aurora A and B. It demonstrates significant antitumor activity against triple-negative breast cancer (TNBC) by reducing cell viability, promoting apoptosis, and inhibiting colony and mammosphere formation in TNBC cells. In vivo studies indicate that KW-2450 free base effectively suppresses the growth of TNBC xenografts, leading to apoptotic cell death or survival of polyploid cells. Additionally, it enhances the therapeutic efficacy of combination treatments with MEK inhibitors, providing a synergistic antitumor effect in various TNBC models.
  24. FLT3 Inhibitor

    AFG206 is a first-generation ATP-competitive "type II" inhibitor of FLT3. This compound effectively inhibits cell proliferation with an IC50 of approximately 0.1 µM by inducing apoptosis in FLT3-ITD-Ba/F3 and D835Y-Ba/F3 cell lines. AFG206 holds significant promise for research applications related to acute myeloid leukemia.
  25. IRAK4 Inhibitor

    Emavusertib phosphate is a potent inhibitor of IRAK4, exhibiting an IC50 of 57 nM. This compound effectively disrupts NF-κB and MyD88 signaling pathways, leading to a significant reduction in pro-inflammatory cytokines such as IL-6 and IL-10. Emavusertib phosphate demonstrates both anti-inflammatory and anti-proliferative effects on cancer cells, promoting apoptosis and showcasing antitumor activity in preclinical mouse models. Its applications extend to investigating inflammatory diseases and cancer therapies.
  26. IRAK4 Inhibitor

    Emavusertib maleate is a potent inhibitor of IRAK4, demonstrating an IC50 of 57 nM, and FLT3. This orally bioavailable compound inhibits NF-κB and MyD88 signaling pathways, effectively reducing the production of pro-inflammatory cytokines such as IL-6 and IL-10. Its anti-inflammatory and anti-proliferative properties make it a valuable tool for cancer research, promoting apoptosis in cancer cells and demonstrating antitumor activity in preclinical mouse models.
  27. IRAK4 Inhibitor

    Emavusertib tosylate is a potent inhibitor of IRAK4, displaying an IC50 of 57 nM. By targeting IRAK4 and FLT3, it effectively disrupts NF-κB and MyD88 signaling pathways, resulting in the reduction of pro-inflammatory cytokines such as IL-6 and IL-10. This compound demonstrates significant anti-inflammatory and anti-proliferative properties against cancer cells, promoting apoptotic mechanisms. Additionally, Emavusertib tosylate has shown noteworthy antitumor activity in preclinical mouse models, making it a valuable reagent for cancer research and inflammation studies.
  28. FLT3 Inhibitor

    BPR1J-340 is a potent inhibitor of FLT3, exhibiting an IC50 of approximately 25 nM. It effectively inhibits the phosphorylation of FLT3 and STAT5, inducing apoptosis in FLT3-ITD positive acute myeloid leukemia (AML) cells. This compound demonstrates considerable anti-tumor activities, making it a valuable tool for research in cancer biology and therapeutic strategies targeting FLT3 dysregulation.
  29. VEGFR2 Inhibitor

    YLL545 is a potent inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2), effectively blocking VEGF-induced phosphorylation of VEGFR2 and preventing the activation of downstream signaling mediators such as phosphorylated STAT3 and phosphorylated ERK1/2 in human umbilical vein endothelial cells (HUVEC). This compound demonstrates significant anti-angiogenic properties by suppressing the proliferation, migration, and invasion of HUVEC. Furthermore, YLL545 has shown the capability to induce apoptosis in breast cancer models and inhibit tumor growth, making it a valuable tool for cancer research and the study of angiogenesis.
  30. FLT3 Inhibitor

    Tandutinib sulfate is a selective inhibitor of FLT3, exerting its effects with an IC50 of 0.22 μM. It also targets c-Kit and PDGFR, with IC50 values of 0.17 μM and 0.20 μM, respectively. This compound is particularly relevant for research in acute myelogenous leukemia (AML) and is noted for its capacity to cross the blood-brain barrier, expanding its potential applications in hematological malignancies and central nervous system studies.
  31. IRAK4 Inhibitor

    Emavusertib mesylate is a potent inhibitor of IRAK4, demonstrating an IC50 of 57 nM. This orally active compound effectively disrupts the NF-κB and MyD88 signaling pathways, leading to a reduction in pro-inflammatory cytokines such as IL-6 and IL-10. Emavusertib mesylate displays anti-inflammatory and anti-proliferative properties against cancer cells, promoting apoptosis. Additionally, it has shown significant antitumor activity in mouse models, making it valuable for cancer research and therapeutic studies targeting inflammatory pathways.
  32. VEGFR2 Inhibitor

    VEGFR-2-IN-18 is a potent inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR-2) with an IC50 of 60 nM. This compound induces apoptosis in targeted cells and exhibits significant antitumor activity. It is a valuable reagent for research applications focused on angiogenesis, cancer biology, and the development of targeted therapies.
  33. c-Met Inhibitor

    LAH-1 is a potent inhibitor of c-Met, demonstrating oral bioavailability and favorable membrane permeability with an IC50 of 49 nM. It exhibits significant anticancer activity by inducing apoptosis and inhibiting cellular migration and invasion. This compound is useful in research applications focused on cancer therapeutics and the modulation of c-Met signaling pathways.
  34. 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.
  35. FGFR Inhibitor

    FGFR-IN-8 is a potent pan-FGFR inhibitor that targets both wild-type and mutant forms of fibroblast growth factor receptors (FGFRs). With impressive inhibitory potency, it demonstrates IC50 values of less than 0.5 nM against FGFR1, V564F-FGFR2, and FGFR3, alongside 22.6 nM for V555M-FGFR3, and 7.30 nM for FGFR4. This compound induces apoptosis in cancer cells and exhibits notable anticancer properties, making it a valuable reagent for cancer research and therapeutic studies involving FGFR signaling pathways.
  36. 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.
  37. 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.
  38. IGF-1R Inhibitor

    KW-2450 tosylate is a selective inhibitor of the insulin-like growth factor-1 receptor (IGF-1R), as well as Aurora A and B kinases. It effectively induces apoptosis in cancer cells, demonstrating significant anticancer activity, particularly against triple-negative breast cancer. This compound is valuable for research applications involving cancer biology and therapeutic targeting of kinase signaling pathways.
  39. 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.
  40. FLT3 Inhibitors

    FLT3-IN-32 is a highly selective, orally bioavailable inhibitor of the FLT3 receptor tyrosine kinase. It effectively targets FLT3-activating mutations, promoting apoptosis in malignant cells. In vivo studies demonstrate significant anti-tumor efficacy in MV4-11 xenograft models within NOD/SCID mice, leading to notable extensions in survival. FLT3-IN-32 is valuable for research applications focused on acute myeloid leukemia.
  41. 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.
  42. VEGFR-2 Inhibitor

    VEGFR-2-IN-23 is a highly selective inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR-2), exhibiting an IC50 value of 0.34 nM. This compound demonstrates significant antitumor activity by inducing apoptosis and causing cell cycle arrest at the G1 phase. VEGFR-2-IN-23 is particularly relevant for research focused on oncology and angiogenesis, providing valuable insights into therapeutic strategies targeting vascular growth pathways.
  43. TRK Inhibitor

    TRK-IN-32 is a potent inhibitor of TRK proteins, effectively targeting TRKWT, TRKG595R, and TRKG667C with IC50 values of 0.08 nM, 2.14 nM, and 0.68 nM, respectively. This compound exhibits significant antiproliferative activity against Ba/F3 cell lines expressing various TRK fusion proteins, including wild type and mutant forms. TRK-IN-32 also induces apoptosis in Ba/F3-TRKAWT and Ba/F3-TRKAG667C cells, making it a valuable tool for investigating the role of TRK signaling in a range of cancers, including thyroid cancer and secretory breast carcinoma.
  44. c-Met Kinase Inhibitor

    c-Met-IN-10 is a highly potent inhibitor of the c-Met kinase, exhibiting an IC50 value of 16 nM. This compound demonstrates significant inhibitory activity against various cancer cell lines, including A549, H460, and HT-29, with IC50 values ranging from 0.56 to 1.59 μM. c-Met-IN-10 effectively suppresses colony formation in HT-29 cells, induces apoptosis in HT-29 and A549 cells, and inhibits A549 cell motility. This reagent is valuable for research applications focused on cancer biology and therapeutic interventions targeting c-Met pathways.
  45. FLT3 Inhibitor

    HSB401 is an orally active FLT3 inhibitor with IC50 values of 28, 5, 72, and 51 nM for FLT3-WT, FLT3-D835Y, FLT3-ITD-F691L, and FLT3-ITD, respectively. It effectively downregulates FLT3 signaling, leading to cell cycle arrest and apoptosis in sensitive cells. Notably, HSB401 spares c-KIT inhibition, minimizing the risk of myelosuppression. This compound has demonstrated significant tumor growth suppression in the MV4-11 xenograft mouse model and is valuable for research in acute myeloid leukemia.
  46. 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.
  47. c-Met Inhibitor

    c-Met-IN-14 is a selective inhibitor of the c-Met kinase, classified as an N-sulfonylamidine derivative, with an IC50 value of 2.89 nM. This compound effectively inhibits c-Met phosphorylation, leading to the arrest of the cell cycle at the G2/M phase and demonstrating significant anticancer activity. Additionally, c-Met-IN-14 induces apoptosis in A549 lung cancer cells in a dose-dependent manner, making it a valuable tool for cancer research and therapeutic studies targeting c-Met signaling pathways.
  48. TRK Inhibitor

    TRK-IN-23 is a selective TRK inhibitor demonstrating potent biological activity with IC50 values of 0.5 nM, 9 nM, 14 nM, 4.4 nM, and 4.8 nM against TRKA, TRKC, TRKAG595R, TRKAF589L, and TRKAG667C, respectively. This compound effectively induces apoptosis in Ba/F3 cells expressing TRKAG595R and TRKAG667C. TRK-IN-23 is valuable for researchers investigating TRK signaling pathways and potential therapeutic interventions in TRK-driven malignancies.
  49. FLT3 Inhibitor

    SILA-123 is a potent FLT3 inhibitor, demonstrating IC50 values of 2.1 nM for FLT3-WT and 1.0 nM for FLT3-ITD. This compound effectively inhibits FLT3 phosphorylation and disrupts downstream signaling pathways, resulting in apoptosis through cell cycle arrest in the G0/G1 phase. SILA-123 is particularly valuable in research related to acute myeloid leukemia.
  50. 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.

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