SGC-GAK-1

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Chemical Structure| 2226517-76-4 同义名 : -
CAS号 : 2226517-76-4
货号 : A1142890
分子式 : C18H17BrN2O3
纯度 : 99%+
分子量 : 389.243
MDL号 : MFCD31689258
存储条件：

Pure form Keep in dark place,Sealed in dry,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 40 mg/mL(102.76 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
描述 GAK (Cyclin G-associated kinase) is a 160 kDa serine/threonine kinase originally identified as a direct association partner of cyclin G. It belongs to the numb-associated kinase (NAK) family and is ubiquitously expressed and within the cell localizes to the Golgi complex, cytoplasm, and nucleus. SGC-GAK-1 is a potent and selective GAK (cyclin G-associated kinase) inhibitor with Ki value of 3.1nM. It exhibited selectivity with IC50 value of 120nM in a NanoBRET target engagement assay and antiproliferative effect on LNCaPa and 22Rv1a with IC50 values of 0.65μM and 0.17μM, respectively, post 72h.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.57mL

0.51mL

0.26mL

12.85mL

2.57mL

1.28mL

25.69mL

5.14mL

2.57mL
参考文献

[1]Asquith CRM, Berger BT, et al. SGC-GAK-1: A Chemical Probe for Cyclin G Associated Kinase (GAK). J Med Chem. 2019 Mar 14;62(5):2830-2836.