AZD1208

For research use only.

Catalog No.S7104

29 publications

AZD1208 Chemical Structure

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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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. 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.
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]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MOLM16 cells NFficm9Rem:uaX\ldoF1cW:wIHHzd4F6 NXv3d4Z2PzJiaB?= NXXDeGZQSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNU2xOOTZiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JGNmdGxiVHn0[ZIuSmy3ZTDhd5NigSxiR1m1NF0xNjB{IN88US=> MmL6NlI4Ojd4NEC=

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
Cleaved PARP / Myc / p-PRAS40 / PRAS40 / p-S6 / p-4EBP1 / 4EBP1 / p-BAD / BAD; 

PubMed: 27270648     


AZD1208-resistant AML cell lines demonstrate sustained mTOR signaling upon treatment. Cells were treated for 4, 24, and 48 hours with 1 μM AZD1208 followed by western blot analysis (n = 3). 

p-MKK4 / p-p38 / p-MK2 / p-AKT ; 

PubMed: 27270648     


The p38 signaling pathway is activated upon AZD1208 treatment. OCI-M1 and OCI-M2 cells were treated with 2 μM AZD1208 for 4, 24, and 48 hours. Cell lysates were harvested and subjected to western blot analysis (n = 3). 

27270648
Immunofluorescence
p-Chk2; 

PubMed: 29879757     


Cells were treated with AZD1208 and AZD5363 alone or in combination for 5 days, and immunofluorescence analysis was subsequently performed. Confocal microscopy was used to observe the signals corresponding to p-Chk2 (red) and γ-H2AX (green). DAPI (blue) was used as a nuclear counterstain. CI, combination index. Scale bars=5 μm.

29879757
Growth inhibition assay
Cell viability; 

PubMed: 30654529     


93T449 and SW872 cells were treated with AZD1208 or vehicle control (DMSO; 0.1%) at the indicated concentrations and for the indicated times. The numbers of surviving cells were measured by cell count assay. The cell count assay was performed in triplicate. Data are means ± SE of three independent experiments. * p < 0.05 compared to the value of AZD1208 free control at the indicated time.

30654529
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
in solvent
Synonyms N/A
Smiles C1CC(CN(C1)C2=C(C=CC=C2C3=CC=CC=C3)C=C4C(=O)NC(=O)S4)N

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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

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

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Frequently Asked Questions

  • Question 1:

    What is your recommended solvent of S7104 for mouse in vivo studies by oral administration?

  • Answer:

    1%CMC-Na is recommended and you will get a suspension. It is ok for oral administration.

  • Question 2:

    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.

selleck catalog

Pim Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID