AZD1208

Catalog No.S7104

AZD1208 Chemical Structure

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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2 Customer Reviews

  • 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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Biological Activity

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.
Targets
Pim1 [1]
(Cell-free assay)
Pim3 [1]
(Cell-free assay)
Pim2 [1]
(Cell-free assay)
0.4 nM 1.9 nM 5 nM
In vitro

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. [1]

In vivo AZD1208 suppresses the growth of MOLM-16 and KG-1a xenograft tumors in vivo in a dose proportional manner. [1]

Protocol

Solubility (25°C)

In vitro DMSO 75 mg/mL warmed (197.63 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 379.48
Formula

C21H21N3O2S

CAS No. 1204144-28-4
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01588548 Completed Advanced Solid Malignancies|Malignant Lymphoma AstraZeneca July 2012 Phase 1
NCT01489722 Terminated Acute Myeloid Leukemia AstraZeneca February 2012 Phase 1

Tech Support

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    I would like to ask which solvent I should use to dissolve AZD1208 for mouse study. Can AZD1208 be dissolved in 5% dextrose?

  • Answer:

    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.

Related Antibodies

Pim Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID