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SGX523
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SGX523图片
CAS NO:1022150-57-7
包装:Free Sample 0.5 mg, 2mg, 5mg, 10mg, 25mg, 50mg, 100mg
包装与价格:
包装价格(元)
Free Sample 0.5 mg电议
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍

生物活性

SGX-523是一种选择性的Met抑制剂,IC50为4 nM,对BRAFV599E, c-Raf, Abl和p38α无抑制活性。SGX-523属于c-Met/肝细胞生长因子受体 (HGFR) 酪氨酸激酶抑制剂,使MET处于失活状态而不能接近其他蛋白激酶。SGX523有效抑制纯化的MET催化区,而不是紧密相关的受体酪氨酸激酶RON。SGX523是ATP竞争性抑制剂,作用于低活性和非磷酸化的MET时亲和力更高(MET-KD(0P), Ki= 2.7 nM)。


化学数据

分子量359.41
分子式C18H13N7S
CAS号1022150-57-7
纯度99.43%
溶解性(25°C)DMSO 10 mg/mL
储存和运输条件固体粉末: -20°C 冷藏长期储存
常温运输及临时存放

实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)

细胞实验
细胞系MDCK cells and A549 cells line (migration)
方法Scatter and Migration Assays
To measure the effect of SGX523 on HGF-induced cell scatter, MDCK cells were plated at 1 × 103per well in a 24-well plate and incubated at 37°C in 5% CO2 for 1 week in MEM and 10% fetal bovine serum. HGF (90 ng/mL) and various concentrations of SGX523 were added, and the cells were incubated for 18 h (37°C, 5% CO2 humidified incubator) and visualized. To investigate cell migration, A549 cells were plated in 12-well plates (6 × 104per well) and incubated to confluence. A channel was introduced into the monolayers by scratching with a pipette tip. Various dilutions of compound were added in starve medium in the presence and absence of HGF (90 ng/mL). Twenty-four hours later, wells were checked for cell migration. Cells were stained and visualized as described.
浓度0, 0.04, 0.12, 0.36 and 3 μ M
处理时间18h or 24h

动物实验
动物模型Human GTL16 tumor xenografts in mice / U87MG tumor xenografts in mice
配制20% isopropanol, 200 mmol/L ammonium acetate, and 100 mmol/L Tris-HCl (pH 7.5); 25% (v/v) glycerol
剂量10, 20, 30, and 100 mg/kg twice daily or 60 mg/kg daily starting at day 4 for 14 d / 10 or 60 mg/kg twice daily starting at day 5 for 22 d
给药处理oral gavage

不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

小鼠大鼠豚鼠仓鼠
重量 (kg)0.020.151.80.40.0810
体表面积 (m2)0.0070.0250.150.050.020.5
Km系数36128520
动物 A (mg/kg) = 动物 B (mg/kg) × 动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。


储备液配制

以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass1 mg5 mg10 mg
1 mM2.7823 mL13.9117 mL27.8234 mL
5 mM0.5565 mL2.7823 mL5.5647 mL
10 mM0.2782 mL1.3912 mL2.7823 mL