Angiogenesis

Items 1201-1250 of 1698

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Product Name
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  1. FLT3 Inhibitor

    TTT 3002 is a potent FLT3 inhibitor that effectively targets FLT3 phosphorylation in the presence of activating mutations at residue D835, demonstrating an IC50 of 0.2 nM. This compound is valuable for research in acute myeloid leukemia (AML) and other related hematologic malignancies. Its specificity and efficacy make it a crucial tool for investigating FLT3 signaling pathways and developing targeted therapies.
  2. FLT3/ITD Mutation Inhibitor

    HP1142 is a selective inhibitor of the FLT3 receptor tyrosine kinase, specifically targeting the FLT3/ITD mutation. This compound, derived from a benzoimidazole scaffold, demonstrates significant efficacy in inhibiting FLT3 signaling pathways. HP1142 is primarily utilized in research focused on FLT3/ITD mutated leukemia, providing valuable insights into therapeutic strategies for this malignancy.
  3. FLT3/CDK4 Inhibitor

    FLT3/CDK4-IN-1 is a highly selective, orally active dual inhibitor targeting FLT3 and CDK4, demonstrating IC50 values of 11 nM and 7 nM, respectively. This compound exhibits significant antiproliferative activity against specific cancer cell lines and shows promising antitumor effects in vivo. FLT3/CDK4-IN-1 is suitable for research applications focused on cancer biology, particularly in exploring pathways associated with leukemias and solid tumors.
  4. PDGFRα/FLT3 Inhibitor

    PDGFRα/FLT3-ITD-IN-2 is a selective inhibitor targeting PDGFRα and FLT3, exhibiting IC50 values greater than 20 μM and 1.654 μM, respectively. This compound demonstrates significant biological activity relevant to the treatment of acute myeloid leukemia and chronic eosinophilic leukemia. Its efficacy in modulating these pathways makes it a valuable tool for investigational research in cancer therapeutics.
  5. PDGFR/TEL-PDGFR/FLT3/KIT Inhibitor

    AGL 2043 is a potent inhibitor of PDGFR, TEL-PDGFR, FLT3, and KIT kinases, exhibiting an IC50 value of 0.8 μM against PDGFR. This compound demonstrates significant biological activity by effectively reducing porcine cardiac smooth muscle cell proliferation and mitigating balloon-induced vascular stenosis. AGL 2043 presents promising applications in the development of anti-restenotic and anticancer therapies.
  6. FLT3/IRAK1/4 Inhibitor

    NCGC1481 is a potent inhibitor of FLT3, IRAK1, and IRAK4, displaying IC50 values of <0.5 nM, 22.6 nM, and 0.8 nM, respectively. This compound effectively mitigates the adaptive resistance of leukemia cells to FLT3 inhibitors, demonstrating significant antileukemic activity. NCGC1481 is suitable for research focused on leukemia treatment and the modulation of key signaling pathways involved in cancer cell survival and proliferation.
  7. FLT3 Inhibitor

    Flt-3 Inhibitor III is a selective inhibitor of the FLT3 kinase with a potent IC50 value of 50 nM. This compound demonstrates minimal activity against other kinases, thereby ensuring specificity. Flt-3 Inhibitor III is primarily utilized in research applications related to cancer biology, particularly in studies investigating FLT3 mutations in acute myeloid leukemia (AML). Its ability to inhibit FLT3 activity underscores its potential as a therapeutic agent in targeted cancer therapies.
  8. MERTK/FLT3 Inhibitor

    MRX-2843 hydrochloride is an orally active, ATP-competitive inhibitor targeting MERTK and FLT3 tyrosine kinases. It demonstrates potent enzymatic inhibitory activity with IC50 values of 1.3 nM for MERTK and 0.64 nM for FLT3. This compound is ideal for research applications investigating cancer therapies and related signaling pathways involving these kinases.
  9. FLT3 Inhibitor

    AAE871 is a potent type I FLT3 inhibitor, exhibiting an IC50 value of 0.034 µM. It demonstrates significant biological activity in inhibiting FLT3 signaling, making it a valuable tool for investigating acute myeloid leukemia (AML) and related hematological malignancies. AAE871 is useful in preclinical studies aimed at understanding FLT3-mediated pathways and their role in cancer progression.
  10. FLT3 Inhibitor

    FLT3-IN-38 is a selective FLT3 inhibitor that targets the FLT3 receptor tyrosine kinase, which is implicated in hematologic malignancies. This compound also exhibits off-target effects by inhibiting serine/threonine kinase haspin, a critical regulator of mitotic signaling. FLT3-IN-38 is suitable for cancer research applications, particularly in studies focused on the treatment of FLT3-mutated leukemias.
  11. ALK Tyrosine Kinase Inhibitor

    Ceritinib-d7 is a deuterium-labeled derivative of Ceritinib, which functions as a selective and ATP-competitive inhibitor of the ALK (anaplastic lymphoma kinase) tyrosine kinase. This compound is utilized in research to explore mechanisms of ALK-mediated oncogenesis and to evaluate the therapeutic efficacy of targeted treatments in malignancies such as non-small cell lung cancer. Its deuterium labeling allows for advanced studies in pharmacokinetics and metabolism, making it a valuable tool for chemical biology investigations.
  12. ALK Inhibitor

    ALK-IN-24 is a potent, orally active inhibitor of anaplastic lymphoma kinase (ALK) with an IC50 value of 1.7 nM, also exhibiting inhibition of insulin receptor kinase with an IC50 value of 6 nM. It effectively suppresses the proliferation of lung adenocarcinoma cells and has demonstrated the ability to inhibit ALK-driven tumor growth in xenograft mouse models. This compound is applicable for research focused on non-small cell lung cancer and other ALK-related malignancies.
  13. ALK/IR/VEGFR2/TIE2/DLK Inhibitor

    CEP-14083 is an ATP-competitive inhibitor targeting ALK, with IC50 values of 2 nM in enzymatic assays. This compound also inhibits other kinases, including the insulin receptor (IR), vascular endothelial growth factor receptor 2 (VEGFR2), angiopoietin-1 receptor (TIE2), and dual leucine zipper kinase (DLK). CEP-14083 has been shown to suppress CD274 mRNA expression and the function of NPM/ALK in NPM/ALK-positive T cell lymphoma cells. It is a valuable tool for research focused on lymphoma and related signaling pathways.
  14. VEGFR-2 Inhibitor

    VS 8 is a potent oral inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR-2), exhibiting significant anti-angiogenic properties. This compound promotes apoptosis in cancer cells and inhibits cellular migration, making it relevant for studies targeting tumor progression. Additionally, VS 8 demonstrates activity against cancer stem cells (CSCs), providing insights for research in cancer treatment and therapeutic resistance.
  15. FLT3 Inhibitor

    FLT3-IN-14 is a potent inhibitor of the FLT3 receptor, exhibiting IC50 values of 5.6 nM for wild-type FLT3 and 1.4 nM for the FLT3-ITD mutant. This compound effectively reduces the phosphorylation of FLT3 at Y591, leading to cell cycle arrest in the G1 phase and subsequent induction of apoptosis. In preclinical studies, FLT3-IN-14 has demonstrated significant efficacy in reducing tumor growth within MV4-11 xenograft mouse models, highlighting its potential for therapeutic applications in FLT3-related malignancies.
  16. EGFR/HER2/TS Inhibitor

    EGFR/HER2/TS-IN-1 is a selective inhibitor targeting EGFR, HER2, and thymidylate synthase (TS) with IC50 values of 0.203 μM, 0.088 μM, and 0.168 μM, respectively. This compound is effective in inducing apoptosis in MCF7 breast cancer cells, making it a valuable tool for cancer research. Its ability to simultaneously inhibit multiple targets renders it a promising candidate for exploring therapeutic strategies in malignancies characterized by overactive EGFR and HER2 signaling pathways.
  17. FGFR4 Inhibitor

    FGFR4-IN-7 is a covalent reversible inhibitor of Fibroblast Growth Factor Receptor 4 (FGFR4), exhibiting an IC50 of 0.42 μM. This compound disrupts the FGFR4 signaling pathway, leading to the induction of apoptosis. FGFR4-IN-7 is primarily utilized in research focused on hepatocellular carcinoma (HCC) and offers potential insights into therapeutic strategies targeting this malignancy.
  18. EGFR Inhibitor

    EGFR-IN-150 is a potent inhibitor of the epidermal growth factor receptor (EGFR), effectively blocking phosphorylation of mutant EGFR and downstream AKT signaling, leading to antitumor activity. This compound demonstrates an IC50 of 0.386 μM in the non-small cell lung cancer (NSCLC) cell line H1975, significantly reducing colony formation and migration in both H1975 and A549 cells while promoting apoptosis. Furthermore, EGFR-IN-150 exhibits substantial tumor growth suppression in the H1975 cell-derived xenograft (CDX) mouse model, making it a valuable tool for research focused on non-small cell lung cancer.
  19. EGFR Inhibitor

    Erbstatin is an inhibitor of the epidermal growth factor receptor (EGFR), targeting its kinase activity to impede downstream signaling pathways. This compound exhibits significant antineoplastic properties, making it a valuable reagent in cancer research. Erbstatin is utilized in studies investigating the role of EGFR in tumor progression and response to therapy, providing insights into potential treatment strategies for EGFR-mediated malignancies.
  20. Tubulin/VEGFR Inhibitor

    Tubulin/VEGFR-2-IN-2 is an orally active inhibitor targeting tubulin and VEGFR-2, exhibiting IC50 values of 3.27 μM and 0.09 μM, respectively. This compound demonstrates significant antitumor activity by enhancing reactive oxygen species generation, disrupting mitochondrial membrane potential, inducing apoptosis, and arresting the cell cycle. Additionally, Tubulin/VEGFR-2-IN-2 possesses anti-angiogenic effects, impairing endothelial cell migration, invasion, and tube formation in vitro. It effectively suppresses angiogenesis, tumor growth, and metastasis in vivo, making it a valuable tool for research involving non-small cell lung cancer, breast cancer, gastric cancer, and lymphoma.
  21. 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.
  22. 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.
  23. 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.
  24. 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.
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. 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.
  32. 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.
  33. 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.
  34. HIF-1α Inhibitor

    GEM-5 is a gemcitabine-based conjugate that functions as a potent HIF-1α inhibitor, with an IC50 value of 30 nM. This compound effectively down-regulates HIF-1α expression while promoting the up-regulation of the tumor suppressor protein p53. GEM-5 has demonstrated the ability to induce apoptosis in A2780 cancer cells and inhibit tumor growth, making it a valuable tool for cancer research and therapeutic studies targeting hypoxia-driven tumor progression.
  35. 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.
  36. 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.
  37. 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.
  38. Bcr-Abl1 Inhibitor

    Radotinib dihydrochloride is a selective Bcr-Abl1 tyrosine kinase inhibitor with an IC50 of 34 nM, demonstrating oral bioavailability and the ability to penetrate the blood-brain barrier. This compound exhibits significant anti-tumor activity by inhibiting cell proliferation, inducing cell cycle arrest, and promoting apoptosis in tumor cells. Radotinib dihydrochloride is utilized in research related to chronic myeloid leukemia, multiple myeloma, and neurodegenerative disorders, particularly those involving prion diseases.
  39. BCR-ABL Inhibitor

    CHMFL-48 is a potent BCR-ABL kinase inhibitor that effectively targets both wild-type and imatinib-resistant mutants. With IC50 values of 1 nM for ABL wild-type and 0.8 nM for the ABL T315I mutant, CHMFL-48 inhibits autophosphorylation of BCR-ABL, disrupting downstream signaling pathways involving STAT5 and CRKL. This mechanism results in cell cycle arrest and the induction of apoptosis, making CHMFL-48 a valuable tool for research focused on chronic myeloid leukemia (CML).
  40. 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.
  41. BCR-ABL Inhibitor

    HS-438 is a potent and selective inhibitor of BCR-ABL, a fusion protein associated with chronic myeloid leukemia (CML). This compound exhibits significant antiproliferative effects, leading to reduced phosphorylation of BCR-ABL at Tyr177, and promotes apoptosis alongside G0/G1 cell cycle arrest. HS-438 demonstrates substantial antitumor activity, making it a valuable tool for investigations into CML and related therapeutic strategies.
  42. 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.
  43. 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.
  44. FAK Signaling Inhibitor

    FAK-IN-5 is a potent inhibitor of focal adhesion kinase (FAK) signaling. It effectively induces apoptosis and autophagy in various cell types, making it a valuable tool for studying cellular responses to FAK modulation. This compound is utilized in cancer research and investigations related to cell migration and survival pathways.
  45. 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.
  46. 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.
  47. 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.
  48. EML4-ALK PROTAC Degrader

    Pro-PEG3-BA is a targeted PROTAC degrader that specifically degrades EML4-ALK and EGFR mutants, with DC50 values of 0.42 μM and 13.50 μM, respectively. It effectively inhibits proliferation and induces cell cycle arrest and apoptosis in non-small cell lung cancer (NSCLC) cell lines in vitro. In vivo studies reveal that Pro-PEG3-BA rewires the ubiquitin-proteasome system, leading to a reduction in EML4-ALK protein levels while demonstrating a favorable safety profile. This reagent is suitable for research focused on non-small cell lung cancer treatments.
  49. EGFRvIII Epitope

    EGFRvIII peptide is a synthetic epitope derived from the EGFRvIII variant, specifically designed to bind to MHC I molecules. This peptide is known to induce apoptosis and elicit targeted immune responses against glioblastoma, particularly when used in conjunction with Flagellin B. It is a valuable tool for research in cancer immunotherapy and the development of personalized medicine approaches for glioblastoma treatment.
  50. 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.

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