Tie-2 억제제/작용제 (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.

Cat.No. 제품명 정보 제품 사용 인용 제품 검증
S1577 Tie2 kinase inhibitor 1 Tie2 kinase inhibitor 1은 SB-203580의 최적화된 화합물로, Tie2에 선택적이며 IC50은 0.25 μM으로 p38보다 200배 더 강력합니다.
Front Pharmacol, 2024, 15:1290128
Protein Cell, 2023, 14(5):350-368
Cancer Lett, 2022, S0304-3835(22)00005-2
Verified customer review of Tie2 kinase inhibitor 1
S1361 MGCD-265 analog MGCD-265는 c-MetVEGFR1/2/3의 강력한 다중 표적 ATP 경쟁적 억제제로, 각각 1 nM, 3 nM/3 nM/4 nM의 IC50을 가집니다. 또한 Ron 및 Tie2를 억제합니다. 임상 1/2상.
Cancer Cell, 2022, S1535-6108(22)00312-9
Cell Rep Med, 2022, 3(1):100492
Protein Cell, 2019, 10(3):161-177
Verified customer review of MGCD-265 analog
S7799 Pexmetinib Pexmetinib은 HEK-293 세포주에서 IC50이 4 nM/18 nM인 강력하고 경구 생체 이용 가능한 이중 p38 MAPK/Tie-2 억제제입니다. 1상.
J Bone Oncol, 2022, 35:100439
Theranostics, 2021, 11(4):1626-1640
Sci Rep, 2021, 11(1):5752
S6412 Altiratinib Altiratinib (DCC-2701)은 TRK, Met (c-Met), TIE2 및 VEGFR2 키나아제의 강력한 한 자리 나노몰 억제제이며, TRKA, B 및 C에 대해 각각 0.9 nM, 4.6 nM 및 0.8 nM의 IC50 값을 가집니다. 이 화합물은 0.3-6 nM 범위의 IC50 값으로 Met (c-Met) 및 Met (c-Met) 돌연변이를 억제합니다.
J Microbiol, 2025, 63(2):e2409001
Theranostics, 2021, 11(20):9918-9936
Cold Spring Harb Mol Case Stud, 2021, 7(5)a006109