Tie-2

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Tie-2 Products

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Catalog No. Product Name Information Product Use Citations Product Validations
S1361 MGCD-265 analog MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of c-Met and VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4 nM, respectively; also inhibits Ron and Tie2. Phase 1/2.
Cell Rep Med, 2022, 3(1):100492
Elife, 2019, 8e47460
Protein Cell, 2019, 10(3):161-177
S1577 Tie2 kinase inhibitor Tie2 kinase inhibitor is an optimized compound of SB-203580, selective to Tie2 with IC50 of 0.25 μM, 200-fold more potent than p38.
Cancer Lett, 2022, S0304-3835(22)00005-2
Int J Mol Sci, 2020, 21(24)E9544
Front Pharmacol, 2019, 10:1373
S6412 Altiratinib Altiratinib (DCC-2701) is a potent single-digit nanomolar inhibitor of TRK, Met (c-Met), TIE2, and VEGFR2 kinases with IC50 vaules of 0.9 nM, 4.6 nM, and 0.8 nM for TRKA, B, and C, respectively. It inhibits Met (c-Met) and Met (c-Met) mutant with IC50 values in the range of 0.3-6 nM.
Theranostics, 2021, 11(20):9918-9936
Cold Spring Harb Mol Case Stud, 2021, 7(5)a006109
S7799 Pexmetinib (ARRY-614) Pexmetinib (ARRY-614) is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with IC50 of 4 nM/18 nM in a HEK-293 cell line. Phase 1.
Theranostics, 2021, 11(4):1626-1640
Sci Rep, 2021, 11(1):5752
J Pharmacol Exp Ther, 2019, 370(2):219-230
S1361 MGCD-265 analog MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of c-Met and VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4 nM, respectively; also inhibits Ron and Tie2. Phase 1/2.
Cell Rep Med, 2022, 3(1):100492
Elife, 2019, 8e47460
Protein Cell, 2019, 10(3):161-177
S1577 Tie2 kinase inhibitor Tie2 kinase inhibitor is an optimized compound of SB-203580, selective to Tie2 with IC50 of 0.25 μM, 200-fold more potent than p38.
Cancer Lett, 2022, S0304-3835(22)00005-2
Int J Mol Sci, 2020, 21(24)E9544
Front Pharmacol, 2019, 10:1373
S6412 Altiratinib Altiratinib (DCC-2701) is a potent single-digit nanomolar inhibitor of TRK, Met (c-Met), TIE2, and VEGFR2 kinases with IC50 vaules of 0.9 nM, 4.6 nM, and 0.8 nM for TRKA, B, and C, respectively. It inhibits Met (c-Met) and Met (c-Met) mutant with IC50 values in the range of 0.3-6 nM.
Theranostics, 2021, 11(20):9918-9936
Cold Spring Harb Mol Case Stud, 2021, 7(5)a006109
S7799 Pexmetinib (ARRY-614) Pexmetinib (ARRY-614) is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with IC50 of 4 nM/18 nM in a HEK-293 cell line. Phase 1.
Theranostics, 2021, 11(4):1626-1640
Sci Rep, 2021, 11(1):5752
J Pharmacol Exp Ther, 2019, 370(2):219-230
Tags: Tie-2 signaling | TEK kinase activty | Tie-2 kinase activty | Tie-2 pathway | Tie-2 phosphorylation | Tie2 signaling pathway | Tie-2 inhibitor review