JAK/Stat

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  1. EGFR inhibitor

    Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations.
  2. EGFR/HER2 oncogenic mutants inhibitor

    Mobocertinib succinate (TAK-788 succinate) is a potent and orally active inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, with selectivity over WT EGFR. Antitumor activity.
  3. EGFR tyrosine kinase inhibitor

    AG-1478 hydrochloride (Tyrphostin AG-1478 hydrochloride) is a selective EGFR tyrosine kinase inhibitor with IC50 of 3 nM.
  4. TYK2 inhibitor

    GDC046 (Compound 3) is a potent, selective, and orally bioavailable inhibitor of TYK2 with Ki of 4.8 nM, 83.8 nM, 27.6 nM and 253 nM for TYK2, JAK1, JAK2, and JAK3, respectively.
  5. JAK3/STAT5 inhibitor

    BD750, an effective immunosuppressant and a JAK3/STAT5 inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation, with IC50 values of 1.5 μM and 1.1 μM in mouse and human T cells, respectively.
  6. Anticancer agent

    BDTX-189 is a potent, orally active and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, including EGFR/HER2 exon 20 insertion mutants. BDTX-189 shows KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. Anticancer activity.
  7. EGFR inhibitor

    Alflutinib is an EGFR inhibitor that targets both EGFR activating mutations and T790M, thus leading to tumor growth inhibition.
  8. EGFR inhibitor

    AG1557 is a specific and ATP competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, has a pIC50 value of 8.194.
  9. FLK-1 (VEGFR-2) / HER2 inhibitor

    SU5204, a tyrosine kinase inhibitor, has IC50s of 4 and 51.5 μM for FLK-1 (VEGFR-2) and HER2, respectively.
  10. TYK2 inhibitor

    RO495 (CS-2667) is a potent inhibitor of Non-receptor tyrosine-protein kinase 2 (TYK2).
  11. EGFT/HER2 inhibitor

    Mobocertinib (TAK-788) is a potent and orally active inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, with selectivity over WT EGFR. Antitumor activity.
  12. JAK2 inhibitor

    TG-89 is an inhibitor of JAK2 with IC50 of 11.2 μM.
  13. VEGFR2 and EGFR signalling inhibitor

    ZD-4190 is a potent, orally available inhibitor of the vascular endothelial cell growth factor receptor 2 (VEGFR2) and of epidermal growth factor receptor (EGFR) signalling, used for the treatment of cancer.
  14. EGFR inhibitor

    Cyasterone, a natural EGFR inhibitor, mainly isolated from Ajuga decumbens Thunb (Labiatae).
  15. dual inhibitor for c-Met and EGFR

    Norcantharidin (Endothall anhydride) is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers.
  16. AK-STAT3 signaling pathway inhibitor

    Ganoderic acid A can inhibit of the JAK-STAT3 signaling pathway, also inhibit proliferation, viability, ROS.
  17. Pdia3/ERp57 activator, STAT3 inhibitor

    Diosgenin palmitate, also known as Diosgenin hexadecanoate, is the hexadecanoic ester of Diosgenin. Diosgenin, a phytosteroid sapogenin, is the product of hydrolysis by acids, strong bases, or enzymes of saponins, extracted from the tubers of Dioscorea wild yam, such as the Kokoro.
  18. EGFR inhibitor

    Mutated EGFR-IN-1 (Osimertinib analog) is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant and T790M resistance mutant.
  19. Pim kinase inhibitor

    TP-3654 is a second-generation Pim kinase inhibitor with Ki values of 5 and 42 nM for Pim-1 and Pim-3, respectively.
  20. T790M-Containing EGFR Mutants inhibitor

    PF-06459988 is an irreversible inhibitor of T790M-Containing EGFR Mutants.
  21. EGFR antagonist

    NRC-2694 is an epidermal growth factor receptor (EGFR) antagonist with anti-cancer and anti-proliferative properties.
  22. JAK3 inhibitor

    JAK3-IN-1 is a potent JAK3 inhibitor with IC50 of 4.8 nM, also inhibits JAK1 (IC50 = 896 nM) and JAK2 (IC50 = 1050 nM).
  23. EGFR inhibitor

    Naquotinib mesylate (ASP8273 mesylate) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.
  24. EGFR/HER2 inhibitor

    Tarloxotinib bromide (TH-4000) is an irreversible EGFR/HER2 inhibitor.
  25. Microtubule-Targeting Agent

    ENMD-119 is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity, and is suitable for inhibiting HIF-1α and STAT3 in human HCC cells.
  26. Pim kinase inhibitor

    GDC-0339 is a potent, orally bioavailable and well tolerated pan-Pim kinase inhibitor, with Kis of 0.03 nM, 0.1 nM and 0.02 nM for Pim1, Pim2 and Pim3, respectively. GDC-0339 is discovered as a potential treatment of multiple myeloma.
  27. Raf/EGFR inhibitor

    Lifirafenib (BGB-283) is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRafV600E and EGFR, respectively.
  28. EGFR inhibitor

    Mutant EGFR inhibitor is a potent and selective mutant EGFR inhibitor extracted from patent WO 2013014448 A1; inhibits EGFRL858R, EGFRExon 19 deletion and EGFRT790M.
  29. JAK1/2/3 inhibitor

    JAK-IN-1 is a JAK1/2/3 inhibitor with IC50s of 0.26, 0.8 and 3.2 nM, respectively. JAK-IN-1 shows improved selectivity for JAK3 over JAK1.
  30. EGFR/HER2/HER4 inhibitor

    BGB-102 is a potent multi-kinase inhibitor against EGFR, HER2, and HER4 with IC50s of 9.6 nM, 18 nM and 40.3 nM, respectively.
  31. JAK2 inhibitor

    NVP-BSK805 dihydrochloride (BSK805 dihydrochloride) is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively.
  32. Pim inhibitor

    INCB053914 phosphate is an inhibitor of Pim extracted from patent WO 2017044730 A1, compound 1; has an IC50 of less than 35 nM.
  33. TYK2 JH2 inhibitor

    Tyk2-IN-7 (Compound 48) is a TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC50 and Ki.app of 0.00053 μM and 0.00007 μM, respectively.
  34. EGFR inhibitor

    TAS6417 is an EGFR inhibitor and an efficacious drug candidate for patients with NSCLC, with IC50 values ranging from 1.1-8.0 nM.
  35. STAT3 inhibitor

    inS3-54A18 is a potent STAT3 inhibitor, with anti-cancer properties.
  36. JAK inhibitor

    JAK-IN-5 is an inhibitor of JAK extracted from patent US20170121327A1, compound example 283.
  37. SYK/JAK inhibitor

    Gusacitinib (ASN-002) is a potent dual inhibitor of spleen tyrosine kinase (SYK) and janus kinase (JAK) with IC50 values of 5-46 nM.
  38. fluorescent probe

    JAK2 JH2 Tracer is a fluorescent probe for the JAK2 JH2 domain, with Kd of 0.2 μM.
  39. EGFR inhibitor

    EGFR-IN-5 is a EGFR inhibitor with IC50s of 10.4, 1.1, 34, 7.2 nM for EGFR, EGFRL858R, EGFRL858R/T790M, and EGFRL858R/T790M/C797S, respectively.
  40. STAT5 inhibitor

    STAT5-IN-2 is a STAT5 inhibitor with EC50s of 9 μM and 5 μM in K562 and KU812 cells, respectively. Potent antileukemic effect.
  41. JAK inhibitor

    JAK-IN-3 (compound 22) is a potent JAK inhibitor, with IC50 values of 3 nM, 5 nM, 34 nM and 70 nM for JAK3, JAK1, TYK2 and JAK2, respectively.
  42. JAK inhibitor

    JAK-IN-4 is a prodrug of a JAK inhibitor, effective in murine collagen induced arthritis model.
  43. Tyk2 inhibitor

    Tyk2-IN-5 (compound 6) is a highly potent, selective and orally active Tyk2 inhibitor and targets the JH2 domain, with a Ki of 0.086 nM for Tyk2 JH2 and an IC50 of 25 nM for IFNα.
  44. KAT3B inhibitor

    L002 is a novel potent, specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 uM.
  45. Stat3 inhibitor

    SH5-07 is a hydroxamic acid based Stat3 inhibitor with an IC50 of 3.9 μM in in vitro assay.
  46. Stat3 inhibitor

    BP-1-102 is an orally available, small-molecule inhibitor of transcription factor Stat3, with an IC50 of 6.8 μM.
  47. TYK2/JAK1/JAK2/JAK3 inhibitor

    SAR-20347 is an inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC50s of 0.6, 23, 26 and 41 nM, respectively.
  48. tyrosine kinase inhibitor

    RG13022 is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor with an IC50 of 4 μM.
  49. EGFR inhibitor

    EGFR-IN-7 (compound 34) is a selective and potent EGFR kinase inhibitor extracted from patent WO2019015655A1, has IC50s of 7.92 nM and 0.218 nM for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) respectively, and shows anti-tumor activity.
  50. EGFR inhibitor

    Mutated EGFR-IN-2 (compound 91) is a mutant-selective EGFR inhibitor extracted from patent WO2017036263A1, which potently inhibits single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M (IC50=??1nM) and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. Mutated EGFR-IN-2 shows anti-tumor antivity.

Items 601-650 of 1052

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