Angiogenesis

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  1. IRAK4/FLT3 inhibitor

    Emavusertib, also known as CA-4948 is a potent IRAK4/FLT3 inhibitor with anti-tumor activity. CA-4948 demonstrated good cellular activity in ABC DLBCL and AML cell lines. CA-4948 demonstrated moderate to high selectivity in a panel of 329 kinases as well as exhibited desirable ADME and PK profiles including good oral bioavailability in mice, rat, and dog and showed >90% tumor growth inhibition in relevant tumor models with excellent correlation with in vivo PD modulation.
  2. Bcr-Abl1 inhibitor

    Vodobatinib, also known as K-0706, is a novel 3rd generation (3G) TKI effective against wild-type and mutated BCR-ABL1 with limited off-target activity.
  3. FGFR/PDGFR/IGF-1R inhibitor

    SU4984 is a cell-permeable, reversible, and ATP-competitive inhibitor of the tyrosine kinase activity of fibroblast growth factor receptor 1 (FGFR1; IC50 = 10-20 μM).

  4. PDGFR inhibitor

    Seralutinibm, also known as PK-10571 and GB002, is a Inhaled Pdgfr Kinase Inhibitor.
  5. FGFR inhibitor

    E-7090 is a fibroblast growth factor receptor inhibitor potentially for the treatment of solid tumors.
  6. 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.
  7. T790M-Containing EGFR Mutants inhibitor

    PF-06459988 is an irreversible inhibitor of T790M-Containing EGFR Mutants.
  8. 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.
  9. HIF-2α inhibitor

    HIF-2α-IN-1 is a HIF-2α inhibitor has an IC50 of less than 500 nM in HIF-2α scintillation proximity assay. IC50 value: ?? 500 nM Target: HIF-2α.
  10. 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.
  11. FLT3 inhibitor

    HM-43239 is a Novel Potent Small Molecule FLT3 Inhibitor, in Acute Myeloid Leukemia (AML) with FMS-like Tyrosine Kinase 3 (FLT3) Mutations
  12. EGFR/HER2 inhibitor

    Tarloxotinib bromide (TH-4000) is an irreversible EGFR/HER2 inhibitor.
  13. VEGFR2 inhibitor

    VEGFR-2-IN-5 is a VEGFR2 inhibitor extracted from patent WO2013055780A1, Page 31.
  14. 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.
  15. ALK/TRKA/TRKB/TRKC inhibitor

    Belizatinib is an oral, dual, potent inhibitor of ALK and TRKA, TRKB, and TRKC, with IC50 of 0.7?nM for wild-type recombinant ALK kinase.
  16. HIF1α inhibitor

    EL102 is a inhibitor of HIF1α , Which can inhibit tubulin polymerisation and decreased microtubule stability.
  17. ALK inhibitor

    X-376 is a potent and highly specific ALK tyrosine kinase inhibitor (TKI) (IC50=0.61 nM). X-376 is a less potent inhibitor of MET (IC50=0.69 nM). X-376 displays potent anti-tumor activity.
  18. HIF-1α inhibitor

    AFP464, is an active HIF-1α inhibitor with an IC50 of 0.25 μM, also is a potent aryl hydrocarbon receptor (AhR) activator.
  19. ATP-competitive multitargeted kinase inhibitor

    Ilorasertib (ABT-348) is a potent and ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora C, Aurora B, and Aurora A with IC50s of 1 nM, 7 nM, 120 nM, respectively.
  20. 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.
  21. VEGFR2 inhibitor

    BIBF 1202 is the carboxylate metabolite of BIBF 1120 which inhibits VEGFR2 kinase with an IC50 of 62 nM.
  22. BTK inhibitor

    Tirabrutinib (ONO-4059) is a highly selective, orally bioavailable BTK inhibitor with an IC50 of 2.2 nM.
  23. BCR-ABL inhibitor

    BCR-ABL-IN-2 is an inhibitor of BCR-ABL1 tyrosine kinase, with IC50s of 57 nM, 773 nm for ABL1native and ABL1T315I, respectively.
  24. dual FLT3/Aurora kinase inhibitor

    CCT241736 is a potent and orally bioavailable dual FLT3 and Aurora kinase inhibitor.
  25. VEGFR inhibitor

    ZK-261991 is an orally active VEGFR tyrosine kinase inhibitor with an IC50 of 5 nM for VEGFR2.
  26. 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.
  27. VEGFR inhibitor

    AG-13958 (AG-013958), a potent VEGFR tyrosine kinase inhibitor, is used for treatment of choroidal neovascularization associated with age-related macular degeneration (AMD).
  28. BTK inhibitor

    GDC-0834 is a potent and selective BTK inhibitor.
  29. 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.
  30. BTK inhibitor

    (R)-Zanubrutinib is the R enantiomer of Zanubrutinib. Zanubrutinib is a selective Bruton tyrosine kinase (BTK) inhibitor.
  31. HIF-2α inhibitor

    (Rac)-PT2399 (Compound 10e), the racemate of PT2399, acts as a potent and specific hypoxia-inducible factor 2a (HIF-2α) inhibitor with an IC50 of 0.01 μM.
  32. c-Met/HGFR inhibitor

    TAS-115 mesylate is a potent VEGFRand hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor, with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively.
  33. 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.
  34. TACC3 inhibitor

    KHS101 hydrochloride could selectively induce a neuronal differentiation phenotype and interacts with transforming acidic coiled-coil-containing protein 3 (TACC3).
  35. Y15

    FAK inhibitor

    Y15 is a potent and specific inhibitor of focal adhesion kinase (FAK) that inhibits its autophosphorylation activity, decreases the viability of cancer cells, and blocks tumor growth.
  36. Raf/VEGFR3 inhibitor

    Sorafenib D3 (Bay 43-9006 D3) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.
  37. Raf/VEGFR3 inhibitor

    Sorafenib D4 (Bay 43-9006 D4) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.
  38. multi-targeted tyrosine kinase inhibitor

    Amuvatinib hydrochloride (MP470 hydrochloride) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret.
  39. KIT and PDGFRA inhibitor

    Avapritinib (BLU-285) is a highly potent, selective, and orally bioavailable KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively.
  40. KIT and PDGFRA switch-control inhibitor

    Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFRA switch-control inhibitor.
  41. 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.
  42. type II PDGFRα kinase inhibitor

    PDGFRα kinase inhibitor 1 is a highly selective type II PDGFRα kinase inhibitor with IC50s of 132 nM and 6115 nM for PDGFRα and PDGFRβ, respectively.
  43. Bcr-Abl inhibitor

    Asciminib (ABL001) is a potent and selective allosteric Bcr-Abl inhibitor; inhibits Ba/F3 cells grown with an IC50 of 0.25 nM.
  44. HIF-1 inhibitor

    GN44028 is a hypoxia inducible factor (HIF)-1 inhibitor, with an IC50 of 14 nM.
  45. ALK/MET inhibitor

    Ensartinib (X-396) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively.
  46. Bcr-Abl kinase inhibitor

    CT-721 is a potent and time-dependent Bcr-Abl kinase inhibitor with an IC50 of 21.3 nM for wild-type Bcr-Abl kinase, and possesses anti-chronic myeloid leukemia (CML) activities.
  47. ALK5/ALK4 inhibitor

    SM 16 is a ALK5/ALK4 kinase inhibitor with Kis of 10 and 1.5 nM, respectively.
  48. FLT3/BTK inhibitor

    CG-806 is an orally active, potent and non-covalent pan-FLT3/pan-BTK inhibitor with an IC50 of 0.08 μM for FLT3. CG-806 has an IC50 of 11 nM against FLT3 wild type (WT)-transfected Ba/F3 cells.
  49. BTK inhibitor

    ARQ 531 is a reversible non-covalent inhibitor of Bruton??s Tyrosine Kinase (BTK), with IC50s of 0.85 nM and 0.39 nM for WT-BTK and C481S-BTK, respectively.
  50. 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.

Items 351-400 of 1495

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