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Tie-2 Inhibitors (4)


Cat.No. Product Name Information Product Use Citation Customer Product Validation
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.
  • Neoplasia, 2012, 14(2):131-40
S1119 Cabozantinib (XL184, BMS-907351) Cabozantinib (XL184, BMS-907351) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively.
  • Cancer Discov, 2014, 4(7):816-27
  • Nat Commun, 2014, 5:3116
  • Mol Cancer Ther, 2014, 10.1158/1535-7163.MCT-14-0274
S1361 MGCD-265 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 Lett, 2013, 340(1):43-50
  • Int J Clin Exp Pathol, 2013, 6(10):2082-91
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.

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S1577 Tie2 kinase inhibitor <1 mg/mL 35 mg/mL <1 mg/mL
S1119 Cabozantinib (XL184, BMS-907351) <1 mg/mL 100 mg/mL <1 mg/mL
S1361 MGCD-265 <1 mg/mL 104 mg/mL <1 mg/mL
S7799 Pexmetinib (ARRY-614) <1 mg/mL 100 mg/mL 100 mg/mL
Tags: Tie-2 signaling | TEK kinase activty | Tie-2 kinase activty | Tie-2 pathway | Tie-2 phosphorylation | Tie2 signaling pathway | Tie-2 inhibitor review
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