SR-3029

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Chemical Structure| 1454585-06-8 同义名 : -
CAS号 : 1454585-06-8
货号 : A662677
分子式 : C23H19F3N8O
纯度 : 99%+
分子量 : 480.45
MDL号 : MFCD30187527
存储条件：

Pure form Keep in dark place, sealed in dry, 2-8°C

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

DMSO: 30 mg/mL(62.44 mM)，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
生物活性
靶点

  • CK1

    CK1δ, IC50:44 nM

    CK1ε, IC50:260 nM
描述 SR-3029 is a strong inhibitor of CK1δ/CK1ε, with IC50 values of 44 nM and 260 nM, respectively. It competes with ATP, having Kis of 97 nM for CK1δ/CK1ε. SR-3029 also inhibits CDK6/cyclin D3, CDK6/cyclin D1, CDK4/cyclin D3, CDK4/cyclin D1, and FLT3, with IC50s of 427, 428, 368, 576, and 3000 nM, respectively. It exhibits inhibitory activity on A375 cells, with an EC50 of 86 nM[1]. SR-3029's efficacy is lower against MCF7 and T47D breast cancer cells, as well as the MCF10A cell line, all of which have low CK1δ expression[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.08mL

0.42mL

0.21mL

10.41mL

2.08mL

1.04mL

20.81mL

4.16mL

2.08mL
参考文献

[1]Bibian M, et al. Development of highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitors with potent antiproliferative properties. Bioorg Med Chem Lett. 2013 Aug 1;23(15):4374-80.

[2]Rosenberg LH, et al. Therapeutic targeting of casein kinase 1δ in breast cancer. Sci Transl Med. 2015 Dec 16;7(318):318ra202.