Tie-2

信号通路图

研究领域

抑制剂选择性比较

Tie-2产品

所有产品(4) Tie-2抑制剂(4)

目录号	产品描述	文献引用	实验数据
S1361	MGCD-265 analog MGCD-265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。	Elife, 2019, 8e47460 Protein Cell, 2019, 10(3):161-177 Mol Cancer Ther, 2018, 17(7):1526-1539	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 inhibitor Tie2 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。	Cancer Sci, 2018, 109(12):3805-3815 Neoplasia, 2012, 14(2):131-40	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).
S6412	Altiratinib Altiratinib (DCC-2701) 是有效的TRK, Met (c-Met), TIE2和VEGFR2激酶抑制剂，对TRKA, B和C的IC50分别为0.9 nM, 4.6 nM和0.8 nM。它抑制Met (c-Met)和Met (c-Met)突变体的IC50范围为0.3-6 nM。
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。	J Pharmacol Exp Ther, 2019, 370(2):219-230

目录号	产品描述	文献引用	实验数据
S1361	MGCD-265 analog MGCD-265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。	Elife,2019, 8e47460 Protein Cell,2019, 10(3):161-177 Mol Cancer Ther,2018, 17(7):1526-1539	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 inhibitor Tie2 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。	Cancer Sci,2018, 109(12):3805-3815 Neoplasia,2012, 14(2):131-40	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).
S6412	Altiratinib Altiratinib (DCC-2701) 是有效的TRK, Met (c-Met), TIE2和VEGFR2激酶抑制剂，对TRKA, B和C的IC50分别为0.9 nM, 4.6 nM和0.8 nM。它抑制Met (c-Met)和Met (c-Met)突变体的IC50范围为0.3-6 nM。
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。	J Pharmacol Exp Ther,2019, 370(2):219-230

Tags: Tie-2 signaling | TEK kinase activty | Tie-2 kinase activty | Tie-2 pathway | Tie-2 phosphorylation | Tie2 signaling pathway | Tie-2 inhibitor review