NT157 treatment resulted in dose-dependent inhibition of IGF1R activation, suppression of IRS protein expression, inhibition of IGF1-induced AKT activation, but increased ERK activation in NT157-treated cells in vitro.
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产品名称 | IGF-1R ↓ ↑ | Insulin Receptor ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
BMS-536924 |
++
IGF-1R, IC50: 100 nM |
+++
Insulin Receptor, IC50: 73 nM |
MEK,FAK | 98% | |||||||||||||||
GSK1904529A |
+++
IGF-1R, IC50: 27 nM |
+++
Insulin Receptor, IC50: 25 nM |
98+% | ||||||||||||||||
Picropodophyllin |
++++
IGF-1R, IC50: 1 nM |
99%+ | |||||||||||||||||
NVP-AEW541 |
++
IGF-1R, IC50: 0.15 μM |
++
Insulin Receptor, IC50: 0.14 μM |
FLT3 | 99%+ | |||||||||||||||
NVP-ADW742 |
+
IGF-1R, IC50: 0.17 μM |
99% | |||||||||||||||||
GSK1838705A |
+++
IGF-1R, IC50: 2 nM |
++++
Insulin Receptor, IC50: 1.6 nM |
ALK | 99% | |||||||||||||||
BMS-754807 |
++++
IGF-1R, IC50: 1.8 nM |
++++
Insulin Receptor, IC50: 1.7 nM |
99%+ | ||||||||||||||||
Linsitinib |
+++
IGF-1R, IC50: 35 nM |
++
Insulin Receptor, IC50: 75 nM |
99%+ | ||||||||||||||||
AG1024 |
+
IGF-1R, IC50: 7 μM |
+
Insulin Receptor, IC50: 57 μM |
98% | ||||||||||||||||
PQ401 |
+
IGF-1R, IC50: <1 μM |
99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | NT157 treatment resulted in dose-dependent inhibition of IGF1R activation, suppression of IRS protein expression, inhibition of IGF1-induced AKT activation, but increased ERK activation in NT157-treated cells in vitro. These effects were correlated with decreased proliferation and increasing apoptosis of LNCaP cells and increasing G2-M arrest in PC3 cells. NT157 can mediate suppression of IGF1R-mediated survival signaling through the established mechanism for negative feedback of IGF1R signaling: targeting IRS1/2 for serine phosphorylation and subsequent degradation. NT157 displayed little to no effect on the survival of normal melanocytes and fibroblasts. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.43mL 0.49mL 0.24mL |
12.13mL 2.43mL 1.21mL |
24.26mL 4.85mL 2.43mL |
CAS号 | 1384426-12-3 |
分子式 | C16H14BrNO5S |
分子量 | 412.255 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,Store in freezer, under -20°C |
溶解度 |
DMSO: 30 mg/mL(72.77 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |