Angiogenesis

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  1. FAK/PYK2 inhibitor

    PF 431396 is a dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor (IC50 values are 2 and 11 nM respectively).
  2. EGFR Inhibitor

    AST-1306, a novel anilino-quinazoline compound, inhibits the enzymatic activities of wild-type epidermal growth factor receptor (EGFR) and ErbB2 as well as EGFR resistant mutant in both cell-free and cell-based systems.
  3. ALK5 inhibitor

    SB-505124 is a selective inhibitor of transforming growth factor-β type I receptor (ALK5), ALK4 and ALK7 (IC50 values are 47 and 129 nM for ALK5 and ALK4 respectively).
  4. Aurora A/B Kinase inhibitor

    PF-03814735 is a novel, potent and reversible inhibitor of Aurora A/B with IC50of 0.8 nM/5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1. Phase 1.
  5. JAK2 inhibitor

    TG101209, a novel JAK2 inhibitor, has significant in vitro activity in multiple myeloma and displays preferential cytotoxicity for CD45+ myeloma cells.

  6. PI3K Inhibitor

    PP121 is a dual inhibitor of receptor tyrosine kinases (RTKs) (IC50 < 0.02 μM for Abl, Src, VEGFR-2 and PDGFR) and PI 3-K family kinases (IC50 < 0.06 μM for p110α, DNA-PK and mTOR).
  7. EGFR Inhibitor

    BMS 599626 is an orally bioavailable inhibitor of the HER1, HER2 and HER4 tyrosine kinases (IC50=22, 32 and 190 nM, respectively) with potential antineoplastic activity.
  8. HER2/EGFR inhibitor

    TAK-285 is an investigational HER2/EGFR inhibitor that penetrates the CNS in Rats with an Intact Blood Brain Barrier (BBB). TAK-285 has inhibitory activity against HER2 and EGFR kinases with IC50 values for HER2 and EGFR of 17 nmol/L (95% CI 12-24) and 23 nmol/L (95% CI 18-30), respectively.[1]
  9. FGFR/VEGFR2 inhibitor

    LY2874455 is a novel and potent FGFR/VEGFR Inhibitor.
  10. multi-kinase inhibitor

    Cenisertib (AS-703569) is a multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3.
  11. VEGFR/EGFR Inhibitor

    BMS-690514 is a potent and selective inhibitor of epidermal growth factor receptor (EGFR), HER2, and HER4, as well as the VEGF receptor kinases.
  12. multi-kinase inhibitor

    Lestaurtinib (CEP-701;KT-5555) is a multi-kinase inhibitor with potent activity against the Trk family of receptor tyrosine kinases. Lestaurtinib inhibits JAK2, FLT3 and TrkA with IC50s of 0.9, 3 and less than 25 nM, respectively.
  13. EGFR inhibitor

    BIBX 1382 is a cell-permeable pyrimidopyrimidine compound that acts as a potent, reversible, ATP-competitive, and highly selective inhibitor of EGFR.
  14. EGFR inhibitor

    Canertinib dihydrochloride (CI-1033 dihydrochloride) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM.
  15. BTK inhibitor

    CGI1746 is a small-molecule Btk inhibitor chemotype with a new binding mode that stabilizes an inactive nonphosphorylated enzyme conformation.
  16. c-Met/VEGFR-2 inhibitor

    E7050 (also known as golvatinib is an orally bioavailable dual kinase inhibitor of c-Met (hepatocyte growth factor receptor) and VEGFR-2 (vascular endothelial growth factor receptor-2) tyrosine kinases with potential antineoplastic activity.
  17. Bcr-Abl inhibitor

    GNF 2 is a Bcr-abl inhibitor that inhibits proliferation and induces apoptosis in Bcr-abl-expressing cells.
  18. VEGFR1/2/3/PDGFRβ/Kit/RET/Raf-1 inhibitor

    Regorafenib Hydrochloride is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
  19. multi-targeted receptor tyrosine kinases inhibitor

    SU14813 maleate is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.
  20. VEGFR Inhibitor

    SU14813 is an oral, multitargeted tyrosine kinase inhibitor (TKI) targeting vascular endothelial growth factor receptors (VEGFR), platelet-derived growth factor receptors (PDGFR), KIT, and fms-like tyrosine kinase 3 (FLT-3)
  21. c-Met Inhibitor

    MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor.
  22. VEGFR2 inhibitor

    CP-547632 is a novel, potent vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor
  23. ALK inhibitor

    ASP3026 is a novel and selective inhibitor for the ALK kinase. ASP3026 potently inhibited ALK kinase activity and was more selective than crizotinib in a Tyr-kinase panel.
  24. ALK inhibitor

    ALK-IN-1, an analog of AP26113, is an orally-available, potent, and selective inhibitor of ALK with a potency of 0.62 nM against wild-type and activity against a wide range of mutants, including the crizotinib-resistant L1196M line.

  25. EGFR inhibitor

    AG-17 is an inhibitor of EGF receptor kinase with an IC50 value of 460 μM in the human epidermoid carcinoma cell line A431.
  26. VEGFR Inhibitor

    ZM 323881 is a potent and selective inhibitor of the kinase activity of the human vascular endothelial growth factor receptor 2 (VEGFR2/KDR).
  27. VEGFR Inhibitor

    ZM 306416 is a VEGF receptor tyrosine kinase inhibitor that inhibits KDR (IC50 = 100 nM) and Flt (IC50 = 2 uM) tyrosine kinases.
  28. FLT3 inhibitor

    TG-02 is a novel small molecule potent CDK/JAK2/FLT3 inhibitor.
  29. Raf kinase inhibitor

    Sorafenib N-Oxide is a metabolite of Sorafenib, a potent Raf kinase inhibitor.
  30. Syk Inhibitor

    Piceatannol is an anti-inflammatory, immunomodulatory and antiproliferative agent. Inhibits p56lck and syk protein tyrosine kinases and inhibits TNF-induced NF-??B activation and gene expression.
  31. BTK inhibitor

    PCI-33380 is an irreversible Bruton's Tyrosine Kinase (BTK) inhibitor (fluorescent probe).
  32. VEGFR3 Inhibitor

    SAR131675, a potent and selective VEGFR-3-TK inhibitor with antilymphangiogenic, antitumoral, and antimetastatic activities.
  33. PHD inhibitor

    TM6089 is a unique Prolyl Hydroxylase (PHD) inhibitor which stimulates HIF activity without iron chelation and induces angiogenesis and exerts organ protection against ischemia.
  34. CDK/JAK2/FLT3 inhibitor

    SB1317 is a potent inhibitor of Cyclin dependent kinases (CDKs), FMS-like tyrosine kinase-3 (FLT3) and Janus kinase 2 (JAK2) with IC50 values of 13nM, 56nM and 73nM for CDK2, JAK2 and FLT3, respectively.
  35. PYK2/FAK inhibitor

    PF-4618433 shows improved PYK2 potency, reduced p38 activity, and superior overall selectivity relative to the prototype BIRB796.
  36. VEGFR inhibitor

    SKLB610 is a novel potential inhibitor of vascular endothelial growth factor receptor tyrosine kinases inhibits angiogenesis and tumor growth in vivo.
  37. c-Abl/c-Kit/PDGRFβ inhibitor

    Flumatinib mesylate can reduce the expression of C-MYC, HIF-1 a and VEGF in U266 cell line in a time- and dose-dependent manners, so flumatinib mesylate may become a new drug for MM therapy.
  38. VEGFR2/PDGFRβ/EphB4 inhibitor

    JI-101 is an orally active inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor beta (PDGFRβ), and the ephrin B4 receptor B4 (EphB4) with potential antiangiogenic and antineoplastic activities.
  39. VEGFR/PDGFR inhibitor

    TAK-593 is an oral formulation containing a small-molecule receptor tyrosine kinase inhibitor of both vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) with potential antineoplastic activity.
  40. FLT3/CDK inhibitor

    FN-1501 is a potent inhibitor of FLT3 and CDK, with IC50s of 2.47, 0.85, 1.96, and 0.28 nM for CDK2/cyclin A, CDK4/cyclin D1, CDK6/cyclin D1 and FLT3, respectively. FN-1501 has anticancer activity.
  41. Bcr-Abl inhibitor

    NRC-AN-019 is an orally administered tyrosine kinase inhibitor (TKI) of the Bcr-Abl protein-tyrosine kinase. NRC-AN-019 is more effective in inhibiting angiogenic potential and proliferation of both MDAMB231 and HTB20/BT474 cells.
  42. EGFR inhibitor

    Tyrphostin AG 183 inhibits EGFR (epidermal growth factor receptor) tyrosine kinase (IC50 = 800 nM).
  43. Alk2 inhibitor

    ALK2-IN-2 is a potent and selective inhibitor of activin receptor-like kinase 2 (ALK2) with an IC50 of 9 nM, and over 700-fold selectivity against ALK3.
  44. EGFR Inhibitor

    EGFR inhibitor is a cell permeable, 4,6-disubstituted pyrimidine compound that selectively inhibits the EGFR kinase with an IC50 value of 21 nM in vitro and blocks receptor autophosphorylation in cells.
  45. EGFR inhibitor

    Icotinib hydrochloride is a potent and specific epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with an IC(50) of 5 nM, including it's mutants of EGFR(L858R), EGFR(L861Q), EGFR(T790M) and EGFR(T790M, L858R).
  46. ALK inhibitor

    CEP-28122 is a highly potent and selective orally active inhibitor of anaplastic lymphoma kinase with antitumor activity in experimental models of human cancers.
  47. EGFR inhibitor

    CNX-2006 is a potent, mutant-selective EGFR inhibitor with excellent in vitro activity in cells with activating EGFR mutations, as well as in cells harbouring the T790M mutation. CNX-2006 is the prototype for CO-1686, which is currently in a Phase I clinical trial for the treatment of EGFR-mutant lung cancer.
  48. EGFR/HER2/HER4 inhibitor

    Epertinib is a potent, oral, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib shows potent antitumor activity.
  49. VEGFR2/Src inhibitor

    TG 100801 is a VEGFR2 targeting prodrug currently in a clinical trial. The active form is TG100572.
  50. VEGFR2/Src inhibitor

    TG 100572 is VEGFR2 and Src kinase inhibitor.

Items 301-350 of 1495

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