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Formula | C18H17N5O3 |
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Molecular Weight | 351.36 | CAS No. | 677338-12-4 | |
Solubility (25°C)* | In vitro | 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | PIK-90 is a PI3Kα/γ/δ inhibitor with IC50 of 11 nM/18 nM/58 nM, respectively, less potent to PI3Kβ. | ||||||||
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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] |
Kinase Assay:[1] |
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Cell Assay:[2] |
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Animal Study:[4] |
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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
, , Saraswati Sukumar of Johns Hopkins University School of Medicine
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Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
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