產品名稱：PIK-90, Free Base
產品貨號：LC  P-9050
產品規格：10 MG
PIK-90 is a synthetic phosphoinositide 3-kinase (PI3K) inhibitor.  The p110α isoform of PI3K is the primary insulin-responsive PI3K in cultured cells.  Compounds targeting p110α block the acute effects of insulin treatment in vivo.  A p110β inhibitor has no effect on insulin treatment.  Zachary, A., et al.  "A Pharmacological Map of the PI3-K Family Defines a Role for p110α in Insulin Signaling."  Cell 125:  733-747 (2006).
PIK-90 is a class I p110α inhibitor (IC50 = 11 nM).  It also blocks p110γ (IC50 = 18 nM), and to a lesser extent p110δ (IC50 = 58 nM) and p110β (IC50 = 350 nM).  Niedermeier, M., et al.  "Isoform-selective phosphoinositide 3'-kinase inhibitors inhibit CXCR4 signaling and overcome stromal cell-mediated drug resistance in chronic lymphocytic leukemia: a novel therapeutic approach."  Blood 113:  5549-5557 (2009).
PIK-90, PI-103, or IC87114 inactivated PI3K and led to uncontrolled sequential switching from IgG1 to IgE.  Zhang, T.T., et al.  "Genetic or pharmaceutical blockade of p110δ phosphoinositide 3-kinase enhances IgE production."  J. Allergy Clin. Immunol. 122:  811-819 (2008).
PIK-90 induced the proliferative arrest of a panel of glioma cell lines.  Combining PIK-90 and the mTORC1 inhibitor rapamycin induced a profound cell cycle arrest, which is similiar to PI-103 treatment alone.  Fan, Q., et al.  "A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma."  Cancer Cell 9:  341-349 (2006).
PI3K inhibitors (PIK-90 and PI-103) enhanced the cytotoxic effects of radiation in PTEN wild type and mutant glioma cells.  Chen, J.S., et al.  "Characterization of structurally distinct, isoform-selective phosphoinositide 3'-kinase inhibitors in combination with radiation in the treatment of glioblastoma."  Mol. Cancer Ther. 7:  841-850 (2008).
Our PIK-90 product, whose CAS number appears above, is the free base.  The CAS number of the hydrochloride salt is 677338-13-5.
Other CAS numbers previously assigned to PIK-90, namely 1029940-40-6 and 1206911-27-4, have been deleted by CAS and are no longer in use.
Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 0.5 mg/mL with warming; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 20-50 µM buffers, serum, or other additives may increase or decrease the aqueous solubility.  Disposal:  A

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