Tie-2
Sigaling Pathway Map
Research Area
- Inhibitory Selectivity
- Solubility
| Catalog No. | Product Name | Solubility(25°C) | ||
|---|---|---|---|---|
| Water | DMSO | Alcohol | ||
| 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 |
| S1577 | Tie2 kinase inhibitor | <1 mg/mL | 35 mg/mL | <1 mg/mL |
| S7799 | Pexmetinib (ARRY-614) | <1 mg/mL | 100 mg/mL | 100 mg/mL |
- Tie-2 Inhibitors (4)
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| 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. |
Effects of AXL inhibitors on induction of pAKT and rescue of pERK following AXL overexpression. R428, 500 nmol/L; XL184, 3 umol/L; XL880, 100 nmol/L; in the presence or absence of 2 umol/L PLX4720. shAXL is a positive control.
|
|
| S1361 |
MGCD-265MGCD-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. |
c-MET/RON inhibitors restore sensitivity to lapatinib in SK-BR-3-LR cells. The concentration used was 0.1 uM for crizotinib, MGCD-265, XL880, sunitinib, dasatinib, TAE-684, and RON inhibitor I. Columns, means; bars, SEMs (n = 3). The phosphorylation of HER2, AKT and ERK1/2 was determined by Western blotting.
|
|
| S1577 |
Tie2 kinase inhibitorTie2 kinase inhibitor is an optimized compound of SB-203580, selective to Tie2 with IC50 of 0.25 μM, 200-fold more potent than p38. |
Inhibition of SVR (solid line) and MS1-VEGF (dashed line) cell survival by sunitinib (A) and Tie2 kinase inhibitor (B) and dose effect analysis of combined sunitinib and Tie2 kinase inhibitor (C). Cell survival was determined as described in Materials and Methods. Combination indices <1, =1, and >1 denote synergy, additivity, and antagonism, respectively. Values represent mean ?SE (n = 4). |
|
| 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. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| 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. |
Effects of AXL inhibitors on induction of pAKT and rescue of pERK following AXL overexpression. R428, 500 nmol/L; XL184, 3 umol/L; XL880, 100 nmol/L; in the presence or absence of 2 umol/L PLX4720. shAXL is a positive control.
|
|
| S1361 |
MGCD-265MGCD-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. |
c-MET/RON inhibitors restore sensitivity to lapatinib in SK-BR-3-LR cells. The concentration used was 0.1 uM for crizotinib, MGCD-265, XL880, sunitinib, dasatinib, TAE-684, and RON inhibitor I. Columns, means; bars, SEMs (n = 3). The phosphorylation of HER2, AKT and ERK1/2 was determined by Western blotting.
|
|
| S1577 |
Tie2 kinase inhibitorTie2 kinase inhibitor is an optimized compound of SB-203580, selective to Tie2 with IC50 of 0.25 μM, 200-fold more potent than p38. |
Inhibition of SVR (solid line) and MS1-VEGF (dashed line) cell survival by sunitinib (A) and Tie2 kinase inhibitor (B) and dose effect analysis of combined sunitinib and Tie2 kinase inhibitor (C). Cell survival was determined as described in Materials and Methods. Combination indices <1, =1, and >1 denote synergy, additivity, and antagonism, respectively. Values represent mean ?SE (n = 4). |
|
| 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. |
