FGFR

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  1. BCR-ABL inhibitor

    AP24534 (Ponatinib) is a potent multi-kinase and pan-BCR-ABL inhibitor.
  2. VEGFR inhibitor

    BIBF1120 (Vargatef) is a novel triple angiokinase inhibitor that inhibits three growth factor receptors simultaneously: VEGFR, PDGF and FGFR.
  3. VEGFR inhibitor

    Brivanib alaninate (BMS-582664) is a dual tyrosine kinase inhibitor of VEGFR and FGFR signaling.
  4. RTK inhibitor

    Dovitinib is a small-molecule multitargeted receptor tyrosine kinase inhibitor, which inhibits Ba/F3 cells transformed to IL3 independence by ZNF198-FGFR1 or BCR-FGFR1 with IC50 values of 150 nM and 90 nM, respectively.
  5. VEGFR-2 inhibitor

    Brivanib (BMS-540215) is a VEGFR -2 inhibitor with an IC50 of 25 nM and Ki of 26 nM.
  6. FLT3/FGFR/Bcr-Abl/Aurora Inhibitor

    KW-2449 is a multikinase inhibitor of FLT3, ABL, ABL-T315I, and Aurora kinase.
  7. VEGFR/PDGFR/FGFR inhibitor

    Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-a/β, and c-kit that blocks tumor growth and inhibits angiogenesis.
  8. FGFR1/VEGFR2 Inhibitor

    PD173074 is a potent, cell permeable and ATP competitive inhibitor of FGFR and VEGFR.
  9. Aurora inhibitor

    Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2
  10. PDFGRβ inhibitor

    Orantinib (TSU-68, SU6668) has greatest potency against PDGFR autophosphorylation with Ki of 8 nM in a cell-free assay, but also strongly inhibits Flk-1 and FGFR1 trans-phosphorylation, little activity against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2; does not inhibit EGFR. Phase 3.
  11. FGFR inhibitor

    AZD4547 is a potent, selective and orally active pan-FGFR inhibitor, with IC50s of 0.2, 2.5, 1.8 and 165 nM for FGFR1, 2, 3 and 4, respectively.
  12. FGFR Inhibitor

    BGJ398 is a potent and selective inhibitor with potential antiangiogenic and antineoplastic activities of fibroblast growth factor receptor (FGFR) tyrosine kinases 1, 2, 3 and 4 (with IC50 values of 0.9, 1.4, 1.0 and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4 respectively).
  13. FGFR/VEGFR2 inhibitor

    LY2874455 is a novel and potent FGFR/VEGFR Inhibitor.
  14. RTK inhibitor

    Dovitinib is a small-molecule multitargeted receptor tyrosine kinase inhibitor, which inhibits Ba/F3 cells transformed to IL3 independence by ZNF198-FGFR1 or BCR-FGFR1 with IC50 values of 150 nM and 90 nM, respectively.
  15. VEGFR inhibitor

    Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-a/β, and c-kit that blocks tumor growth and inhibits angiogenesis.
  16. VEGFR/FGFR/EGFR inhibitor?€?

    SU-5402 is a potent and selective vascular endothelial growth factor receptor (VEGFR) and fibroblast growth factor receptor (FGFR) inhibitor (IC50 values are 0.02, 0.03, 0.51 and > 100 μM at VEGFR2, FGFR1, PDGFRβ and EGFR respectively).
  17. c-Met Inhibitor

    MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor.
  18. FGFR Inhibitor

    FIIN-2 is an irreversible inhibitor of FGFR1-4 with IC50 values of 3.1, 4.3, 27, and 45 nM, respectively.
  19. multi-targeted tyrosine kinase inhibitor

    Tyrosine kinase-IN-1 is a multi-targeted tyrosine kinase inhibitor with IC50s of 4, 20, 4, 2 nM for KDR, Flt-1, FGFR1 and PDGFRα, respectively.
  20. IGF-1R, Aurora, FGFR, ABL, SRC inhibitor

    XL228 is a protein kinase inhibitor targeting IGF1R, the AURORA kinases, FGFR1-3, ABL and SRC family kinases. XL228 is an Aurora A inhibitor (IC50, f3 nmol/L) that has shown potent biochemical activity against ABL1 (Ki, 5 nmol/L), as well as the BCR-ABL1 T315I (Ki, 1.4 nmol/L) kinases.
  21. Chk2, KDR, FGFR, Aurora A & Cdk2 inhibitor

    R1530 is a pyrazolobenzodiazepine small molecule with potential antiangiogenesis and antineoplastic activities. R1530 is also a mitosis-angiogenesis inhibitor (MAI) that inhibits multiple receptor tyrosine kinases involved in angiogenesis, such as vascular endothelial growth factor receptor (VEGFR)-1, -2, -3, platelet-derived growth factor receptor (PDGFR) beta? FMS-like tyrosine kinase (Flt)-3, and fibroblast growth factor receptor (FGFR) -1, -2.
  22. FGFR1 inhibitor

    SSR128129E is an orally-active and allosteric FGFR1 inhibitor with IC50 of 1.9 uM
  23. FGFR1/2/3 inhibitor

    Debio-1347 is an orally bioavailable inhibitor of the fibroblast growth factor receptor subtypes 1 (FGFR-1), 2 (FGFR-2) and 3 (FGFR-3), with potential antineoplastic activity.
  24. FGFR1 inhibitor

    ACTB-1003 is an oral kinase inhibitor targeting cancer mutations (FGFR inhibition), angiogenesis (inhibition of VEGFR2 and Tie-2) and induces apoptosis (targeting RSK and p70S6K, downstream of PI3 kinase).
  25. VEGFR/FGFR Inhibitor

    E-3810 is a potent and selective dual inhibitor of VEGF and FGF receptors with IC50 values of 7 nM, 25 nM, 10 nM, 17.5 nM and 82.5 nM for VEGFR-1, VEGFR-2, VEGFR-3, FGFR-1 and FGFR-2, respectively.
  26. FGFR Inhibitor

    NVP-BGJ398 phosphate is a novel selective, pan-specific FGFR inhibitor with IC50 of 0.9, 1.4, and 1 nM for FGFR1, FGFR2, and FGFR3, respectively; >40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes.
  27. FGFR inhibitor

    BLU9931 is the first selective small molecule inhibitor of FGFR4 with IC50 of 3 nM; less potent for FGFR1/2/3(IC50> 150 nM),
  28. Irreversible FGFR inhibitor

    FIIN-3 is a potent, selective, irreversible and the next-generation covalent FGFR inhibitor.
  29. FGFR2 Inhibitor

    Alofanib is a potent and selective allosteric inhibitor of FGFR2 with potential anticancer activity.
  30. FGFR inhibitor

    Erdafitinib is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity.
  31. RTK inhibitor

    Nintedanib is a potent inhibitor of multiple receptor tyrosine kinases (RTKs) and non-receptor tyrosine kinases (nRTKs).
  32. FGFR4 inhibitor

    FGFR4-IN-1 is a potent inhibiotr of FGFR4 with IC50 of 0.7 nM.
  33. FGFR4 inhibitor

    H3B-6527 is a highly selective FGFR4 inhibitor with potent antitumour activity in FGF19 amplified cell lines and mice.
  34. FGFR inhibitor

    Derazantinib(ARQ-087) is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with IC50 values of 1.8 nM for FGFR2, and 4.5 nM for FGFR1 and 3, showing lower potency for FGFR4 (IC50=34 nM). It also inhibits RET, DDR2, PDGFRβ, VEGFR and KIT.
  35. FGFR inhibitor

    Rogaratinib, also known as BAY-1163877, is an aberrant fibroblast growth factor receptor (FGFR) inhibitor.
  36. FGFR inhibitor

    PD166866 is a FGFR1 inhibitor with IC50 value of 55 nM, and no effect on c-Src, PDGFR-b, EGFR or insulin receptor tyrosine kinases or MEK, PKC, and CDK4.
  37. multi-targeted tyrosine kinase inhibitor

    Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
  38. FGFR1/DDR2 inhibitor

    FGFR1/DDR2 inhibitor 1 is an inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2), with IC50 values of 31.1 nM, 108.4 nM and 3.2 nM for FGFR1, KG-1, and DDR2, respectively.
  39. FGFR/VEGFR inhibitor

    ODM-203 is a potent FGFR and VEGFR families inhibitor with IC50s of 11, 16, 6, 35 nM towards recombinant FGFR1, FGFR2, FGFR3 and FGFR4 as well as 26, 9, 5 nM towards VEGFR1, VEGFR2 and VEGFR3, respectively.
  40. FGFR1-4/CSF1R inhibitor

    PRN1371 is a highly selective and potent FGFR1-4 and CSF1R inhibitor with IC50s of 0.6, 1.3, 4.1, 19.3 and 8.1 nM for FGFR1, FGFR2, FGFR3, FGFR4 and CSF1R, respectively.
  41. FGFR4 inhibitor

    Roblitinib (FGF-401; Compound Example 83) is a highly selective and potent FGFR4 inhibitor with an IC50 of 1.9 nM. Roblitinib has antitumor activity.
  42. FGFR inhibitor

    Pemigatinib is a selective FGFR inhibitor in development for the treatment of patients with cholangiocarcinoma.
  43. SUN11602 is a novel aniline compound with basic fibroblast growth factor-like activity.
  44. FGFR4 inhibitor

    Fisogatinib (BLU-554) is a potent, highly selective and orally active fibroblast growth factor receptor 4 (FGFR4) inhibitor with an IC50 of 5 nM.
  45. FGFR inhibitor

    Futibatinib (TAS-120) is an orally bioavailable, highly selective, and irreversible FGFR inhibitor.
  46. FGFR 1/2/3/4 inhibitor

    ASP5878 is an oral active inhibitor of FGFR 1, 2, 3, and 4, with IC50 values of 0.47 nM, 0.6 nM, 0.74 nM and 3.5 nM for FGFR 1, 2, 3, and 4 kinase activity. ASP5878 has potential antineoplastic activity.
  47. PDGFR/VEGFR/Src inhibitor

    PP58 is a pyrido[2,3-d]pyrimidine-based compound that inhibits PDGFR, FGFR and Src family activities with nanomolar IC50 values.
  48. MET, AXL/MER, and FGFR1/2/3 inhibitor

    S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC50 values below 20 nM.
  49. multi-targeted kinase inhibitor

    ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.
  50. FGFR3 inhibitor

    Dovitinib(CHIR-258; TKI258) lactate is a potent inhibitor of fibroblast growth factor receptor 3 (FGFR3) with an IC50 of 5 nM.

Items 1-50 of 60

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