Tie-2 inhibitors/agonists

As the known endothelial cells specific RTKs along with the vascular endothelial growth factor (VEGF) receptor, Tie-2 belongs to the Tie family of endothelial-specific receptor tyrosine kinases which plays a key role in cell proliferation, migration and survival during angiogensis. Tie-2 is predominantly expressed on vascular endothelial cells and binds all the known angiopoietin (ANGPT) ligands is a receptor for the angiopoietin (ANG) family: ANG-1, ANG-2, and ANG-3. The Tie-2 receptor and the angiopoietins as important regulators of tumor-induced angiogenesis and, therefore, cancer growth and metastasis. Activated Tie-2 activates several other effectors including endothelial nitric oxide synthase (eNOS), SH2 domain-containing phosphatase (SHP2), growth factor receptor-bound protein 2 (GRB2), the p85 subunit of PI3K.

Protein Tyrosine Kinase

Aurora Kinase CDK Chk ROCK Antimetabolites APC Wee1 MPS1 Rho Myc DYRK BMI-1 eIF LIM kinase PFKFB RUNX Nur77 FOXM1 Choline kinase Haspin Kinase Mad2 p21 Cyclin CDK4/6 Cell Cycle Arrest

All (4)
Tie-2 Inhibitors (4)
New Tie-2 Products

Cat.No.	Product Name	Information	Product Use Citations
S1577	Tie2 kinase inhibitor 1	Tie2 kinase inhibitor 1 is an optimized compound of SB-203580, selective to Tie2 with IC50 of 0.25 μM, 200-fold more potent than p38.	Front Pharmacol, 2024, 15:1290128 Protein Cell, 2023, 14(5):350-368 Cancer Lett, 2022, S0304-3835(22)00005-2
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.	Cancer Cell, 2022, S1535-6108(22)00312-9 Cell Rep Med, 2022, 3(1):100492 Protein Cell, 2019, 10(3):161-177
S7799	Pexmetinib	Pexmetinib 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.	J Bone Oncol, 2022, 35:100439 Theranostics, 2021, 11(4):1626-1640 Sci Rep, 2021, 11(1):5752
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. This compound inhibits Met (c-Met) and Met (c-Met) mutant with IC50 values in the range of 0.3-6 nM.	J Microbiol, 2025, 63(2):e2409001 Theranostics, 2021, 11(20):9918-9936 Cold Spring Harb Mol Case Stud, 2021, 7(5)a006109
S1577	Tie2 kinase inhibitor 1	Tie2 kinase inhibitor 1 is an optimized compound of SB-203580, selective to Tie2 with IC50 of 0.25 μM, 200-fold more potent than p38.	Front Pharmacol, 2024, 15:1290128 Protein Cell, 2023, 14(5):350-368 Cancer Lett, 2022, S0304-3835(22)00005-2
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.	Cancer Cell, 2022, S1535-6108(22)00312-9 Cell Rep Med, 2022, 3(1):100492 Protein Cell, 2019, 10(3):161-177
S7799	Pexmetinib	Pexmetinib 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.	J Bone Oncol, 2022, 35:100439 Theranostics, 2021, 11(4):1626-1640 Sci Rep, 2021, 11(1):5752
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. This compound inhibits Met (c-Met) and Met (c-Met) mutant with IC50 values in the range of 0.3-6 nM.	J Microbiol, 2025, 63(2):e2409001 Theranostics, 2021, 11(20):9918-9936 Cold Spring Harb Mol Case Stud, 2021, 7(5)a006109

Tie-2 inhibitors/agonists

Protein Tyrosine Kinase

Signaling Pathway Map