Tie-2
信号通路图
研究领域
- 抑制剂选择性比较
- 溶解性比较
| 目录号 | 产品目录 | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| S1361 | Glesatinib (MGCD265) | <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抑制剂（3）
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1361 |
Glesatinib (MGCD265)Glesatinib (MGCD265)是一种有效的，多靶点，及ATP竞争性的c-Met和VEGFR1/2/3抑制剂，IC50分别为1 nM， 3 nM/3 nM/4 nM，也抑制Ron和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.
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| S1577 |
Tie2 kinase inhibitorTie2 kinase inhibitor是SB-203580的优化产物，选择性作用于Tie2，IC50为0.25 μM，比作用于p38效果高200倍。 |
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). |
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| S7799 |
Pexmetinib (ARRY-614)Pexmetinib (ARRY-614)是一种有效的，口服生物可利用的，双重p38 MAPK/Tie-2抑制剂，其在HEK-293细胞中的IC50分别为4 nM/18 nM。Phase 1。 |
