PKI-402

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Chemical Structure| 1173204-81-3 同义名 : -
CAS号 : 1173204-81-3
货号 : A786338
分子式 : C29H34N10O3
纯度 : 99+%
分子量 : 570.645
MDL号 : MFCD18251484
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: 4 mg/mL(7.01 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
靶点

  • p110γ

    PI3Kγ, IC50:16 nM

  • p110β

    PI3Kβ, IC50:7 nM

  • p110α

    PI3Kα, IC50:2 nM

  • p110δ

    PI3Kδ, IC50:14 nM
描述 PKI-402 is a potent dual pan-PI3K/mTOR inhibitor targeting PI3Kα/β/γ/δ and mTOR with IC50 of 2 nM/7 nM/16 nM/14 nM and 3 nM.
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
MDA-MB-361 cells Function assay 4 h Inhibition of Akt T308 phosphorylation in human MDA-MB-361 cells after 4 hrs by Western blotting, IC50=0.005 μM 19968288
PC3 cells Cytotoxicity assay 72 h Cytotoxicity against human PC3 cells with PTEN mutant after 72 hrs, IC50=0.021 μM 19968288
SF9 insect cells Function assay 2 h Inhibition of human PI3Kalpha expressed in SF9 insect cells after 2 hrs by fluorescence polarization assay, IC50=0.001 μM 21763134
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.75mL

0.35mL

0.18mL

8.76mL

1.75mL

0.88mL

17.52mL

3.50mL

1.75mL
参考文献

[1]Mallon R, Hollander I, et al. Antitumor efficacy profile of PKI-402, a dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor. Mol Cancer Ther. 2010 Apr;9(4):976-84.

[2]Dehnhardt CM, Venkatesan AM, et al. Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: discovery of PKI-402. J Med Chem. 2010 Jan 28;53(2):798-810.