AZD1208
Catalog No.S7104
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.
6 Customer Reviews
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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.
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.
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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.
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(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. | ||||||||||||||||
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| 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 |
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| 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] |
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| Cell Data |
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| 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 |
Bio Calculators
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Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01588548 | Completed | Advanced Solid Malignancies|Malignant Lymphoma | AstraZeneca | July 2012 | Phase 1 |
| NCT01588548 | Completed | Advanced Solid Malignancies|Malignant Lymphoma | AstraZeneca | July 2012 | Phase 1 |
| NCT01489722 | Terminated | Acute Myeloid Leukemia | AstraZeneca | February 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.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.
Frequently Asked Questions
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Question 1:
What is your recommended solvent of S7104 for mouse in vivo studies by oral administration?
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Answer:
1%CMC-Na is recommended and you will get a suspension. It is ok for oral administration.
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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?
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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.
