GDC-0326

产品说明书

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Chemical Structure| 1282514-88-8 同义名 : -
CAS号 : 1282514-88-8
货号 : A129632
分子式 : C19H22N6O3
纯度 : 98%
分子量 : 382.42
MDL号 : MFCD30730064
存储条件：

Pure form Sealed in dry, 2-8°C

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

DMSO: 105 mg/mL(274.57 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

  • p110γ

    PI3Kγ, Ki:10.2 nM

  • p110β

    PI3Kβ, Ki:26.6 nM

  • p110α

    PI3Kα, Ki:0.2 nM

  • p110δ

    PI3Kδ, Ki:4 nM
描述 GDC-0326 is a potent and selective inhibitor of α-Isoform of Phosphoinositide 3-Kinase (PI3Kalpha inhibitor). GDC-0326 achieves a very high level of selectivity over other kinases.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.62mL

0.52mL

0.26mL

13.07mL

2.62mL

1.31mL

26.15mL

5.23mL

2.62mL
参考文献

[1]Soler A, Figueiredo AM, et al. Therapeutic Benefit of Selective Inhibition of p110α PI3-Kinase in Pancreatic Neuroendocrine Tumors. Clin Cancer Res. 2016 Dec 1;22(23):5805-5817.

[2]Heffron TP, Heald RA, et al. The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f] imidazo[1,2-d] [1,4] oxazepin-9-yl)oxy)propanamide (GDC-0326). J Med Chem. 2016 Feb 11;59(3):985-1002.