產品櫥窗
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PIK-90
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產品型號：101-677338-12-4 商品規格： |
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PI3K Inhibitor. Synonym : N-(2,3-dihydro-7,8-dimethoxyimidazo[1,2-c]quinazolin-5-yl)-3-pyridinecarboxamide、PIK-85、PI3-K inhibitor IX
C18H17N5O3
M.W.: 351.4
PIK-90 is a potent and cell permeable phosphoinositide 3-kinase (PI3K) inhibitor. Through this action, PIK-90 reduces chemotaxis and induces apoptosis in chronic lymphocytic leukemia B cells. It also blocks proliferation of glioma cells in vitro.2 By inhibiting P110α, PIK-90 blocks insulin-stimulated phosphorylation of Akt in L1 adipocytes and L6 myotubes, preventing activation of the mTORC1 pathway.
In vitro, PIK-90 also inhibits p110β, p110δ, PI3KC2α, PI3KC2β, hsVPS34, PI4KIIIα, PI4KIIIβ, ATR, ATM and mTORC1 with IC50s of 350 nM, 58 nM, 47 nM, 64 nM, 830 nM, 830 nM, 3.1 μM, 15 μM, 610 nM and 1.05 μM, respectively. To determine the effects of PIK-90 on chronic lymphocytic leukemia (CLL) cell viability, CLL cells from different patients are incubated with various concentrations of PIK-90 (1 μM and 10 μM) for 24, 48, and 72 hours. PIK-90 reveals the strong apoptosis-inducing effects at both concentrations and at all different time points. Using a concentration of 10 μM, PIK-90 reduces the viability of CLL cells to 51.1% plus or minus 6.6% at 24 hours, whereas 1 μM PIK-90 reduces the viability to 77.8% plus or minus 6.4%
Niedermeier, M., Hennessy, B.T., Knight, Z.A., 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(22), 5549-5557 (2009).
Fan, Q.W., Knight, Z.A., Goldenberg, D.D., et al. A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma. Cancer Cell 9(5), 341-349 (2006).
Knight, Z.A., Gonzalez, B., Feldman, M.E., et al. A pharmacological map of the PI3-K family defines a role for p110α in insulin signaling. Cell 125(4), 733-747 (2006).
M.W.: 351.4
PIK-90 is a potent and cell permeable phosphoinositide 3-kinase (PI3K) inhibitor. Through this action, PIK-90 reduces chemotaxis and induces apoptosis in chronic lymphocytic leukemia B cells. It also blocks proliferation of glioma cells in vitro.2 By inhibiting P110α, PIK-90 blocks insulin-stimulated phosphorylation of Akt in L1 adipocytes and L6 myotubes, preventing activation of the mTORC1 pathway.
In vitro, PIK-90 also inhibits p110β, p110δ, PI3KC2α, PI3KC2β, hsVPS34, PI4KIIIα, PI4KIIIβ, ATR, ATM and mTORC1 with IC50s of 350 nM, 58 nM, 47 nM, 64 nM, 830 nM, 830 nM, 3.1 μM, 15 μM, 610 nM and 1.05 μM, respectively. To determine the effects of PIK-90 on chronic lymphocytic leukemia (CLL) cell viability, CLL cells from different patients are incubated with various concentrations of PIK-90 (1 μM and 10 μM) for 24, 48, and 72 hours. PIK-90 reveals the strong apoptosis-inducing effects at both concentrations and at all different time points. Using a concentration of 10 μM, PIK-90 reduces the viability of CLL cells to 51.1% plus or minus 6.6% at 24 hours, whereas 1 μM PIK-90 reduces the viability to 77.8% plus or minus 6.4%
Niedermeier, M., Hennessy, B.T., Knight, Z.A., 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(22), 5549-5557 (2009).
Fan, Q.W., Knight, Z.A., Goldenberg, D.D., et al. A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma. Cancer Cell 9(5), 341-349 (2006).
Knight, Z.A., Gonzalez, B., Feldman, M.E., et al. A pharmacological map of the PI3-K family defines a role for p110α in insulin signaling. Cell 125(4), 733-747 (2006).
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