Molecular Weight(MW): 379.48
AZD1208 is a potent, and orally available Pim kinase inhibitor with IC50 of 0.4 nM, 5 nM, and 1.9 nM for Pim1, Pim2, and Pim3 in cell-free assays, respectively. Phase 1.
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Loss of proliferation in ATL-derived cell lines by the Pim-kinase inhibitor AZD1208 (D). Cell counts were repeated at least twice. Results represent the percentage of cells alive after 5 days of Pim inhibitor treatment, compared with 5 days treated with DMSO. For AZD1208, cells were treated with 0, 5, or 10 μM AZD1208. Normal PBMCs (n = 2) were used as a control. Western blots indicate loss of Pim1 targets, p-4EBP1 (Thr37/46), p-p70S6K (Thr389), and loss of pBad (Ser20) (negligible for Smi-4a) after 24 hours with 0, 5, or 10 μM AZD1208; or DMSO control.
Blood, 2016, 127(20):2439-50.. AZD1208 purchased from Selleck.
(D) IC50 values calculated from cell viability assays of indicated cell lines, with the top concentration for PIM447 and AZD1208 being 10 μM. Shown is the mean of four replicates ± SEM. (E) IC50 values calculated from cell viability assays of indicated cell lines, with the top concentration for AEB071 being 10 μM and 1 μM for Ibrutinib. Shown is the mean of four replicates ± SEM. (F) ABC DLBCL cell lines, grouped based on drug sensitivity, with known somatic mutations.
Oncotarget, 2016, 7(39):63362-63373. AZD1208 purchased from Selleck.
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Choose Selective Pim Inhibitors
|Description||AZD1208 is a potent, and orally available Pim kinase inhibitor with IC50 of 0.4 nM, 5 nM, and 1.9 nM for Pim1, Pim2, and Pim3 in cell-free assays, respectively. Phase 1.|
|Features||Orally bioavailable Pim kinase inhibitor that has been tested in Phase I clinical trials for treatment of advanced solid tumors and malignant lymphoma.|
AZD1208 is an orally available, potent and highly selective Pim inhibitor that effectively inhibits all three isoforms. AZD1208 inhibits the growth of several AML cell lines and sensitivity correlates with the level of Pim-1 expression, STAT5 activation and presence of protein tyrosine kinase mutation. AZD1208 causes cell cycle arrest and apoptosis in MOLM-16 cells in culture. This is accompanied by a dose-dependent reduction in phosphorylation of BAD, 4EBP1 and p70S6K. In addition, AZD1208 leads to potent inhibition of colony growth of primary AML cells from bone marrow aspirates and downregulates phosphorylation of Pim targets. 
|In vivo||AZD1208 suppresses the growth of MOLM-16 and KG-1a xenograft tumors in vivo in a dose proportional manner. |
|In vitro||DMSO||75 mg/mL warmed (197.63 mM)|
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Frequently Asked Questions
I would like to ask which solvent I should use to dissolve AZD1208 for mouse study. Can AZD1208 be dissolved in 5% dextrose?
AZ1208 can be dissolved in 5% dextrose at 10 mg/ml as a suspension. If 5% Tween 80 added, the suspension will be more homogeneously.