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Angiogenesis

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Items 101-150 of 515

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  1. A11235
    PF 573228

    FAK Inhibitor

    PF 573228 is a potent and selective inhibitor of focal adhesion kinase (FAK) (IC50 = 4 nM).
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  2. A11236
    TAK-285

    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]
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  3. A11237
    FG-4592 (Roxadustat)

    HIF-PHs inhibitor

    FG-4592 is a novel hypoxia inducible factor prolyl hydroxylase inhibitor, in CKD anemia.
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  4. A11244
    LY 2874455

    FGFR/VEGFR2 inhibitor

    LY2874455 is a novel and potent FGFR/VEGFR Inhibitor.
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  5. A11262
    Cenisertib

    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.
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  6. A11263
    BMS-690514

    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.
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  7. A11320
    BAY 61-3606

    Syk Inhibitor

    BAY 61-3606 is a cell-permeable imidazopyrimidine compound that acts as a potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase activity with no inhibitory effect against Btk, Fyn, Itk, Lyn, and Src.
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  8. A11334
    BIBX 1382

    EGFR inhibitor

    BIBX 1382 is a cell-permeable pyrimidopyrimidine compound that acts as a potent, reversible, ATP-competitive, and highly selective inhibitor of EGFR.
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  9. A11344
    Canertinib dihydrochloride

    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.
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  10. A11348
    CGI1746

    BTK inhibitor

    CGI1746 is a small-molecule Btk inhibitor chemotype with a new binding mode that stabilizes an inactive nonphosphorylated enzyme conformation.
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  11. A11349
    Cabozantinib S-malate

    multiple receptor tyrosine kinases inhibitor

    Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
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  12. A11350
    CP-673451

    PDGFRα/β inhibitor

    CP 673451 is a potent PDGFR-β inhibitor with an IC50 of 1 nM.
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  13. A11396
    E-7050 (Golvatinib)

    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.
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  14. A11407
    Apatinib (YN968D1)

    VEGFR inhibitor

    Apatinib (YN968D1) is a tyrosine kinase inhibitor that selectively inhibits the vascular endothelial growth factor receptor-2 (VEGFR2, also known as KDR) that inhibits VEGF-mediated endothelial cell migration and proliferation thus blocking new blood vessel formation in tumor tissue.
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  15. A11411
    Dovitinib (TKI-258)

    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.
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  16. A11416
    Erlotinib

    EGFR inhibitor

    Erlotinib is an epidermal growth factor receptor inhibitor (EGFR inhibitor). Erlotinib HCl was approved. Erlotinib binds in a reversible fashion to the adenosine triphosphate (ATP) binding site of the receptor. For the signal to be transmitted, two EGFR molecules need to come together to form a homodimer. These then use the molecule of ATP to trans-phosphorylate each other on tyrosine residues, which generates phosphotyrosine residues, recruiting the phosphotyrosine-binding proteins to EGFR to assemble protein complexes that transduce signal cascades to the nucleus or activate other cellular biochemical processes. When erlotinib binds to EGFR, formation of phosphotyrosine residues in EGFR is not possible and the signal cascades are not initiated.
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  17. A11439
    GNF 2

    Bcr-Abl inhibitor

    GNF 2 is a Bcr-abl inhibitor that inhibits proliferation and induces apoptosis in Bcr-abl-expressing cells.
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  18. A11472
    Ki 20227

    M-CSFR, CSF1R inhibitor

    Ki 20227 is an inhibitor of c-Fms tyrosine kinase (M-CSFR, CSF1R).
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  19. A11496
    Motesanib (AMG706)

    VEGFR Inhibitor

    Motesanib (AMG706) is a multikinase inhibitor that selectively targets VEGF receptors, platelet-derived growth factor receptors (PDGFRs), and Kit receptors with IC?? values of 2 nM (VEGFR1), 3 nM (VEGFR2), 6 nM (VEGFR3), 84 nM (PDGFR), and 8 nM (Kit).
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  20. A11507
    NVP-TAE 226

    FAK inhibitor

    NVP-TAE226 is a potent FAK inhibitor with IC50 of 5.5 nM and modestly potent to Pyk2(IC50=3.5 nM); 10- to 100-fold less potent against InsR, IGF-1R, ALK, and c-Met.
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  21. A11518
    Pazopanib (GW-786034)

    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.
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  22. A11546
    Regorafenib Hydrochloride

    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.
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  23. A11556
    SU14813 maleate

    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.
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  24. A11557
    SU14813

    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)
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  25. A11558
    SU-5402

    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).
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  26. A11581
    Toceranib (PHA 291639, SU 11654)

    c-Kit, PDGFR, VEGFR inhibitor

    Toceranib is a kinase inhibitor with both antitumor and antiangiogenic activity through inhibition of KIT, vascular endothelial growth factor receptor 2, and PDGFRβ.
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  27. A11753
    MK-2461

    c-Met Inhibitor

    MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor.
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  28. A11772
    CP-547632

    VEGFR2 inhibitor

    CP-547632 is a novel, potent vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor
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  29. A11773
    ASP3026

    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.
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  30. A11924
    IOX 2

    HIF-PHD inhibitor

    IOX2 is a potent inhibitor of HIF-1α prolyl hydroxylase-2 (PHD2) with IC50 of 21 nM in a cell-free assay, >100-fold selectivity over JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH.
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  31. A11926
    R788 (Fostamatinib)

    Syk inhibitor

    R788 (Fostamatinib) is an important spleen tyrosine kinase (Syk) inhibitor, showing efficacy against kinase-mediated IgG Fc gamma receptor signaling.
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  32. A11929
    PF-04554878 (Defactinib)

    FAK inhibitor

    PF-04554878 is a novel FAK kinase inhibitor that decreases growth and induces apoptosis in pancreatic neuroendocrine tumor cells
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  33. A11948
    ALK-IN-1 (Brigatinib analog, AP26113 analog)

    ALK inhibitor

    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. In a panel of EML4-ALK or NPM-ALK-positive cell lines, AP26113 has IC50 values of 4-31 nM. [1][2] AP26113 is effective against sensitive and resistant H3122 cells, reducing cell growth, suppressing ALK phosphorylation, and inducing apoptosis. In Ba/F3 cells expressing native or mutant EML4-ALK, AP26113 was active at IC50s of 10 and 24 nM, respectively. [3]
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  34. A11949
    AG-17

    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.
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  35. A11952
    P505-15 (PRT062607, BIIB057)

    Syk inhibitor

    P505-15 (also known as PRT062607) is a novel, highly selective, and orally bioavailable small molecule SYK inhibitor (SYK IC(50) = 1 nM) with anti-SYK activity that is at least 80-fold greater than its affinity for other kinases.
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  36. A11954
    ZM 323881 hydrochloride

    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).
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  37. A11955
    ZM 306416

    VEGFR Inhibitor

    ZM 306416 is a VEGF receptor tyrosine kinase inhibitor that inhibits KDR (IC50 = 100 nM) and Flt (IC50 = 2 uM) tyrosine kinases.
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  38. A11962
    TG-02 (SB1317)

    FLT3 inhibitor

    TG-02 is a novel small molecule potent CDK/JAK2/FLT3 inhibitor.
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  39. A12005
    Sorafenib N-Oxide

    Raf kinase inhibitor

    Sorafenib N-Oxide is a metabolite of Sorafenib, a potent Raf kinase inhibitor.
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  40. A12162
    Piceatannol

    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.
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  41. A12270
    PCI-33380

    BTK inhibitor

    PCI-33380 is an irreversible Bruton's Tyrosine Kinase (BTK) inhibitor (fluorescent probe).
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  42. A12357
    FIIN-2

    FGFR Inhibitor

    FIIN-2 is an irreversible inhibitor of FGFR1-4 with IC50 values of 3.1, 4.3, 27, and 45 nM, respectively.
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  43. A12358
    A 83-01

    TGF-β/ALK5 inhibitor

    A83-01 is a selective inhibitor of the transforming growth factor-beta type I receptor ALK5, the Nodal receptor ALK4, and the nodal receptor ALK7
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  44. A12419
    Go 6976

    PKC inhibitor

    Go6976 is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and Flt3.
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  45. A12421
    CHMFL-ABL/KIT-155

    ABL/c-KIT dual kinase inhibitor

    CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor.
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  46. A12427
    TCS 359

    FLT3 inhibitor

    TCS 359 is a potent inhibitor of FLT3 receptor tyrosine kinase (IC50 = 42 nM) that displays selectivity over a range of other kinases.
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  47. A12437
    SU 5416 (Semaxinib)

    VEGFR Inhibitor

    SU 5416 is an inhibitor of vascular endothelial growth factor receptor (VEGFR) that also inhibits other tyrosine kinases KIT, MET, FLT3 and RET.
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  48. A12472
    SU1498

    VEGFR2 inhibitor

    SU1498 is a selective inhibitor of the VEGFR2; inhibits Flk-1 with an IC50 of value of 700 nM.
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  49. A12486
    Tyrosine kinase-IN-1

    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.
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  50. A12496
    BCR-ABL-IN-1

    BCR-ABL inhibitor

    BCR-ABL-IN-1 is an inhibitor of BCR-ABL tyrosine kinase, with a pIC50 of 6.46, and may be used in the research of chronic myelogenous leukemia.
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