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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Cited by 14 Publications

6 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.

  • Primary AML sample (AML#6) treated with the pan-Pim kinases inhibitors AZD1208 (1 μM) or LGB321 (1 μM). Western blots were done using RSK2, Pim2 and β-actin antibodies.

    Leukemia, 2018, 32(3):597-605. AZD1208 purchased from Selleck.

  • AZD1208-resistant cell lines demonstrate sustained mTOR signaling upon treatment. Cells were treated with 2 μmol/L AZD1208 for 0, 24, and 48 hours, followed by Western blot analysis (n = 3).

    Mol Cancer Ther, 2018, 17(4):849-857. 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.

  • (D) HBL1 cells were plated in 0.9% MethoCult (1,000 cells/well) with vehicle, ibrutinib (100 or 1,000 nM), AZD-1208 (100 or 1,000 nM), or the combinations, and colony formation was scored after 7 days. Graphs represent quantifications of 3 wells, expressed as mean ± SD. (E) HBL1 tumor cells were implanted into CB17 SCID mice, and the indicated drugs were orally administered daily when the tumors reached 150 mm3. Tumors were measured twice a week. Significant tumor suppression was observed in the group treated with the ibrutinib/AZD-1208 combination compared with the vehicle-treated group (*P<0.01, repeated measures MANOVA-adjusted univariate F-test).

    Am J Cancer Res, 2016, 6(11):2489-2501. AZD1208 purchased from Selleck.

  • Effect of the Pim1 inhibitor AZD1208 on the expression of NFIL3 (at 24 h) and viability of eosinophils (at 48 h) stimulated with IL-5 and Dex. A) AZD1208 at a concentration specific for inhibition of Pim1 activity (1ng/ml) blocked upregulation of NFIL3 by IL-5 and Dex/IL-5 (24 h) without a significant effect on Pim1 expression. B) Inhibition of Pim1 activity by AZD1208 blocked the anti-apoptotic effect of IL-5 and restored the proapoptotic effect of Dex on activated eosinophils, * p<0.05 vs. control cells. The error bars represent the standard deviation of 4 experiments from 3 independent donors.

    Apoptosis, 2016, 21(4):421-31. AZD1208 purchased from Selleck.

Purity & Quality Control

Choose Selective Pim Inhibitors

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MOLM16 cells M3ruPXBzd2yrZnXyZZRqd25iYYPzZZk> M{jnb|czKGh? Mm\PRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPT1zNNVYh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPlcIwhXGm2ZYKtRox2\SCjc4PhfUwhT0l3ME2wMlAzKM7:TR?= MoXxNlI4Ojd4NEC=

... 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

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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:

    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.

Pim Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID