产品说明书
GSK1904529A
 |
同义名 : | GSK 4529 |
| CAS号 : | 1089283-49-7 | |
| 货号 : | A417175 | |
| 分子式 : | C44H47F2N9O5S | |
| 纯度 : | 98+% | |
| 分子量 : | 851.963 | |
| MDL号 : | MFCD17010271 | |
| 存储条件： |
粉末 Sealed in dry,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 50 mg/mL(58.69 mM)，配合低频超声助溶，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： |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
|
||
| 描述 | IGF-1R (insulin-like growth factor-1 receptor) plays a key role in transformation, growth and survival of malignant cells, and has been considered as a general and promising target for cancer treatment. GSK1904529A is a selective inhibitor of IGF-IR and IR with IC50 values of 27 and 25nM, respectively. Treatment with GSK1904529A ranging in 0.03-3μM dose-dependently inhibited IGF-1- or insulin-induced autophosphorylation of IGF-1R, as well as the downstream signaling, including phosphorylation of ATK, IRS-1 and ERK. And this inhibition on phosphorylation on IGF-1R and its downstream can be also observed in vivo. In COLO 205, MCF-7, and NCI-H929 cells treated with GSK1904529A ranging in 0.3-10μM for 24h or 48h, dose-dependent increased accumulation in G1 of the cell cycle could be observed. GSK1904529A showed anti-proliferation of cell lines derived from solid and hematologic malignancies, among which multiple myeloma and Ewing’s sarcoma cell lines showed most sensitivity. Oral administration of GSK1904529A at 30mg/kg once daily or twice daily for 21 days significantly inhibited tumor growth inhibition of female nude mice bearing tumor xenografts of NIH-3T3/LISN, COLO 205, HT29 and BxPC3, respectively. As GSK1904529A is also a IR inhibitor, minimal effects on blood glucose levels can be observed in animals treated with a single dose of 30 mg/kg GSK1904529A[1]. | ||
| 作用机制 | GSK1904529A is a reversible, ATP-competitive inhibitor.[1] | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| human COLO205 cells | Proliferation assay | 72 h | Antiproliferative activity against human COLO205 cells after 72 hrs by Celltiter assay, IC50=124 nM | 19101143 | |
| human LP-1 cells | Proliferation assay | 72 h | Antiproliferative activity against human LP-1 cells after 72 hrs by Celltiter assay, IC50=104 nM | 19101143 | |
| human NCI-H929 cells | Proliferation assay | 72 h | Antiproliferative activity against human NCI-H929 cells after 72 hrs by Celltiter assay, IC50=81 nM | 19101143 | |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
1.17mL 0.23mL 0.12mL |
5.87mL 1.17mL 0.59mL |
11.74mL 2.35mL 1.17mL |
