Tie2 kinase inhibitor Chemical Structure
XL-184 free base (Cabozantinib) is a potent multitargeted VEGFR2, Met, FLT3, Tie2, Kit and Ret inhibitor with IC50 of 0.035, 1.8, 14.4, 14.3 and 4.6 nM for VEGFR2, Met, FLT3, Tie2 and Kit, respectively.
MGCD-265 is a multi-targeted kinase inhibitor, which targets the c-MET, VEGFR1, VEGFR2, VEGFR3, Tie-2 and Ron receptor tyrosine kinases.
Linifanib (ABT869) is a structurally novel, potent RTK and VEGF and PDGF receptor families inhibitor for, PDGFR-β, KDR, and CSF-1R, with IC50 of 0.2 nM, 2 nM, 4 nM, and 7 nM, respectively.
Axitinib (AG-013736) is a multiple receptor kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-β and c-KIT with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM, respectively.
Saracatinib (AZD0530) is a Src inhibitor of c-Src with IC50 of 2.7 nM.
BIBF1120 (Vargatef) is a potent VEGF receptor (VEGFR), PDGFR and FGFR kinase inhibitor for VEGFR1, VEGFR2, VEGFR3 with IC50 of 34 nM, 5 nM and 5 nM, respectively.
BIBW2992 (Afatinib, Tomtovok, Tovok) irreversibly inhibits EGFR/HER2 including EGFRwt, EGFR L858R , EGFR L858R/T790M and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM, 14 nM, respectively.
BMS-536924 is a small molecule ATP-competitive IGF-IR kinase inhibitor with with an IC50 of 80 nM.
Bosutinib (SKI-606) is a Src family kinase inhibitor. Inhibited migration of breast cancer cell lines with IC50 values of 0.1 to 0.3 umol/L.
Cediranib (AZD2171) is a highly potent VEGFR2 inhibitor for VEGF-stimulated proliferation and KDR phosphorylation with IC50 of 0.4 nM and 0.5 nM, respectively.
Tie2 kinase inhibitor is a potent, reversible, and ATP-binding site-targeting Tie2 inhibitor with an IC50 of 250 nM. It is a cell-permeable pyridinylimidazole compound. It has ~ 200-fold selectivity over p38 MAPK and greater than 10-fold selectivity over VEGFR2, VEGFR3, and PDGFR1β. It was shown to exhibit antiangiogenesis activity in a Matrigel assay (70% reduction, 50 mg/kg/0.5 day, i.p.) and inhibit the growth of xenografted tumor (no apparent growth up to 20 days, 25 mg/kg/0.5 day, i.p.) in mice in vivo.[1]
| Molecular Weight (WM): | 439.53 |
|---|---|
| Formula: | C26H21N3O2S |
| CAS No.: | 948557-43-5 |
| Synonyms: |
N/A
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| Dissolve in (25°C): | DMSO ≥35mg/mL |
| Water <1mg/mL | |
| Ethanol <1mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
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