Src I1

目录号: GC16957纯度: >99.50%同义词: 7-二甲氧基-N-(4-苯氧基苯基)-氨基喹唑啉,Src Kinase Inhibitor 1; Src-l1
A potent inhibitor of Src kinases

Src I1
Cas No.: 179248-59-0
规格价格库存数量操作
2mg¥350.00现货
1
5mg¥490.00现货
1
10mg¥665.00现货
1
25mg¥1,540.00现货
1
50mg¥2,765.00现货
1
10mM (in 1mL DMSO)¥403.00现货
1

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产品描述 Description

Src Inhibitor 1 is a potent and selective dual site Src tyrosine kinase inhibitor with IC50 values of 44 nM for Src and 88nM for Lck.

Src-I1 is competitive with both ATP and peptide binding sites of the kinase. The IC50 values are 44 and 88 nM for Src and Lck, respectively[1]. Src-I1, is found to be a potent inhibitor of Src (IC50=0.18 μM), but also inhibited other Src family members, such as Lck, Csk and Yes with similar potency to Src, and RIP2 (IC50=0.026 μM) with even greater potency. In addition, it inhibited CHK2 with similar potency to Src, and Aurora B with slightly lower potency[2].

References:
[1]. Tian G, et al. Structural determinants for potent, selective dual site inhibition of human pp60c-src by 4-anilinoquinazolines. Biochemistry. 2001 Jun 19;40(24):7084-91.
[2]. Bain J, et al. The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.

实验参考方法 Experimental Reference Method

Kinase experiment:

Assays (25.5 μL volume) are carried out robotically at room temperature (21°C) and are linear with respect to time and enzyme concentration under the conditions used. Assays are performed for 30 min using Multidrop Micro reagent dispensers in a 96-well format. The concentration of magnesium acetate in the assays is 10 mM and [γ-33P]ATP (800 c.p.m./pmol) is used at 5, 20 or 50 μM as indicated, in order to be at or below the Kmfor ATP for each enzyme.The assays are initiated with MgATP, stopped by the addition of 5 μL of 0.5 M orthophosphoric acid and spotted on to P81 filter plates using a unifilter harvester. The IC50 values of inhibitors are determined after carrying out assays at ten different concentrations of each compound[2].

References:

[1]. Tian G, et al. Structural determinants for potent, selective dual site inhibition of human pp60c-src by 4-anilinoquinazolines. Biochemistry. 2001 Jun 19;40(24):7084-91.
[2]. Bain J, et al. The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
179248-59-0
同义词
7-二甲氧基-N-(4-苯氧基苯基)-氨基喹唑啉,Src Kinase Inhibitor 1; Src-l1
化学名
6,7-dimethoxy-N-(4-phenoxyphenyl)quinazolin-4-amine
SMILES
COC(C=C1C(N=CN=C1NC(C=C2)=CC=C2OC3=CC=CC=C3)=C4)=C4OC
分子式
C22H19N3O3
分子量
373.4 g/mol
溶解性
DMF: 0.25 mg/ml,DMF:PBS(pH7.2) (1:2): 0.33 mg/ml,DMSO: 2.5 mg/ml
保存条件
Store at 2-8°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol