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CAS No. 1204144-28-4
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. AZD1208 induces autophagy, cell cycle arrest and apoptosis. Phase 1.
Selleck's AZD1208 has been cited by 29 publications
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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. AZD1208 induces autophagy, cell cycle arrest and apoptosis. 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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In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
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Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01489722||Terminated||Drug: AZD1208||Acute Myeloid Leukemia||AstraZeneca||February 2012||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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Frequently Asked Questions
What is your recommended solvent of S7104 for mouse in vivo studies by oral administration?
1%CMC-Na is recommended and you will get a suspension. It is ok for oral administration.
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.