PIK-90

製品コードS1187 バッチS118702

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C18H17N5O3
分子量 351.36 CAS No. 677338-12-4
Solubility (25°C)* 体外 DMSO 2 mg/mL (5.69 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 PIK-90 is a PI3Kα/γ/δ inhibitor with IC50 of 11 nM/18 nM/58 nM, respectively, less potent to PI3Kβ.
in vitro PIK-90 shows distinct patterns of isoform selectivity to inhibit different subsets of four class I PI3K isoforms. In addition, PIK-90 completely inhibits the fMLP-stimulated phosphorylation of Akt and impairs polarity and chemotaxis in dHL60 cells. [1] PIK-90 exhibits significantly antiproliferative activity by effectively blocking phosphorylation of Akt in six glioma cell lines varying in mutational status at PTEN or p53, including U87 MG, SF188, SF763, LN229, A1207 and LN-Z30 cells. Moreover, PIK-90 induces a modest G0G1 arrest at a concentration (0.5 μM) sufficient to inhibit phosphorylation of Akt substantially. [2] In chronic lymphocytic leukemia (CLL) cells, PIK-90 inhibits chemotaxis to levels that are 57.8% of controls at 1 μM and 56.8% of controls at 10 μM. Consistently, PIK-90 inhibits pseudoemperipolesis to levels that are 74.2% PIK-90 of controls at 1 μM and 57.9% of controls at 10 μM. In addition, PIK-90 also leads to a significant reduction of CLL cell migration into the stromal cell layer and decreases CXCL12-induced actin polymerization. [3]
in vivo Immediately following insulin treatment, PIK-90 (10 mg/kg) completely protects animals from this insulin-stimulated decline in blood glucose. [4]

プロトコル(参考用のみ)

キナーゼアッセイ Expression and Assay of p110α/p85α, p110β/p85α, p110δ/p85α, and p110γ
IC50 values are measured using either a standard TLC assay for lipid kinase activity or a high-throughput membrane capture assay. Kinase reactions are performed by preparing a reaction mixture containing kinase, inhibitor (2% DMSO final concentration), buffer (25 mM HEPES, pH 7.4, 10 mM MgCl2), and freshly sonicated phosphatidylinositol (100 μg/mL). Reactions are initiated by the addition of ATP containing 10 μCi of γ-32P-ATP to a final concentration 10 μM or 100 μM, and allowed to proceed for 20 minutes at room temperature. For TLC analysis, reactions are then terminated by the addition of 105 μL 1N HCl followed by 160 μL CHCl3:MeOH (1:1). The biphasic mixture is vortexed, briefly centrifuged, and the organic phase transferred to a new tube using a gel loading pipette tip precoated with CHCl3. This extract is spotted on TLC plates and developed for 3-4 hours in a 65:35 solution of n-propanol:1M acetic acid. The TLC plates are then dried, exposed to a phosphorimager screen, and quantitated. For each compound, kinase activity is typically measured at 10-12 inhibitor concentrations representing two-fold dilutions from the highest concentration tested (100 μM). For compounds showing significant activity, IC50 determinations are repeated two to four times, and the reported value is the average of these independent measurements.
細胞アッセイ 細胞株 U87 MG, SF188, SF763, LN229, A1207 and LN-Z3 cells
濃度 0 to 1 μM
反応時間 72 hours
実験の流れ For viabilty, cells are seeded in 12-well plates in the presence of PIK-90 for 3 days. Cell viability is determined using a WST-1 assay.
動物実験 動物モデル FVB/N female mice are fasted at 9:00 a.m. and then given human insulin or vehicle (PBS) intravenously at 12:00 p.m.
投薬量 ≤10 mg/kg
投与方法 Administered via i.p.

カスタマーフィードバック

Data from [Data independently produced by J Biol Chem, 2014, 289(18), 12467-84]

Data from [Data independently produced by J Cell Biol, 2012, 198(2), 185-94]

, , Dr. Yong-Weon Yi from Georgetown University Medical Center

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人間や獣医の診断であるか治療的な使用のためにでない。

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