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7-二甲氧基-N-(4-苯氧基苯基)- 氨基喹唑啉

7-二甲氧基-N-(4-苯氧基苯基)- 氨基喹唑啉用途

Src Inhibitor 1是高效选择性的双位点Src酪氨酸激酶抑制剂，对Src和Lck的IC₅₀值分别为44 nM和88 nM。

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7-二甲氧基-N-(4-苯氧基苯基)- 氨基喹唑啉名称

[ CAS 号 ]:
179248-59-0

[ 中文名 ]:
7-二甲氧基-N-(4-苯氧基苯基)- 氨基喹唑啉

[ 英文名 ]:
Src Inhibitor-1

[英文别名 ]:

Src Kinase Inhikitor
Src Kinase Inhibitor I
Src-l1
Src Inhibitor-1
KIN001-030
Src Inhibitor 1

7-二甲氧基-N-(4-苯氧基苯基)- 氨基喹唑啉生物活性

[ 描述 ]:

Src Inhibitor 1是高效选择性的双位点Src酪氨酸激酶抑制剂,对Src和Lck的IC50值分别为44 nM和88 nM。

[ 相关类别 ]:

信号通路 >> 蛋白酪氨酸激酶 >> SRC

研究领域 >> 癌症

[ 靶点 ]

IC50: 44 nM (Src), 88 nM (Lck)[1]

[体外研究]

Src-I1与激酶的ATP和肽结合位点竞争。对于Src和Lck,IC50值分别为44和88nM [1]。 Src-I1被发现是一种有效的Src抑制剂(IC50 =0.18μM),但也抑制其他Src家族成员,如Lck,Csk和Yes,具有与Src相似的效力,以及RIP2(IC50 =0.026μM)甚至更大的效力。此外,它抑制CHK2具有与Src相似的效力,Aurora B具有略低的效力[2]。

[激酶实验]

测定（25.5μL体积）在室温（21℃）下自动进行，并且在所用条件下相对于时间和酶浓度是线性的。使用96孔格式的Multidrop Micro试剂分配器进行30分钟的测定。测定中乙酸镁的浓度为10mM，并且如所示使用5,20或50μM的[γ-33P] ATP（800cpm / pmol），以使其等于或低于每种酶的Km for ATP。用MgATP引发测定，通过加入5μL的0.5M正磷酸终止测定，并使用单过滤器收集器点在P81滤板上。在以10种不同浓度的每种化合物进行测定后，测定抑制剂的IC 50值[2]。

[参考文献]

[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.

[相关活性小分子]

7-二甲氧基-N-(4-苯氧基苯基)- 氨基喹唑啉物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
528.2±50.0 °C at 760 mmHg

[ 分子式 ]:
C₂₂H₁₉N₃O₃

[ 分子量 ]:
373.405

[ 闪点 ]:
273.2±30.1 °C

[ 精确质量 ]:
373.142639

[ PSA ]:
65.50000

[ LogP ]:
4.90

[ 蒸汽压 ]:
0.0±1.4 mmHg at 25°C

[ 折射率 ]:
1.665

[ 储存条件 ]:
2-8°C

7-二甲氧基-N-(4-苯氧基苯基)- 氨基喹唑啉MSDS

详细MSDS(安全技术说明书)

7-二甲氧基-N-(4-苯氧基苯基)- 氨基喹唑啉安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H315-H319-H335-H413

[ 警示性声明 ]:
P280-P301 + P312 + P330-P305 + P351 + P338-P337 + P313

[ 危险品运输编码 ]:
UN 3077 9 / PGIII

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