AZD1208

Catalog No.S7104 Batch:S710403

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Technical Data

Formula

C21H21N3O2S
Molecular Weight 379.48 CAS No. 1204144-28-4
Solubility (25°C)* In vitro DMSO 75 mg/mL (197.63 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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.
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]
Features Orally bioavailable Pim kinase inhibitor that has been tested in Phase I clinical trials for treatment of advanced solid tumors and malignant lymphoma.

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    MDSCs

  • Concentrations

    1 μM

  • Incubation Time

    4 h

  • Method

    Bone marrow derived MDSCs were separated into M-MDCSs and suppressive neutrophils by FACS, then plated in RPMI with 10% FBS in the presence of DMSO or AZD1208 for 4 hours on coverslips.
Animal Study:

[3]
  • Animal Models

    Female CB17 SCID mice

  • Dosages

    10 & 30 mg/kg

  • Administration

    o.g.

Customer Product Validation

, , Blood, 2016, 127(20):2439-50.

Data from [Data independently produced by , , Leukemia, 2018, 32(3):597-605]

Data from [Data independently produced by , , Mol Cancer Ther, 2018, 17(4):849-857]

Data from [Data independently produced by , , Oncotarget, 2016, 7(39):63362-63373]

Selleck's AZD1208 has been cited by 40 publications

2-Desaza-annomontine (C81) impedes angiogenesis through reduced VEGFR2 expression derived from inhibition of CDC2-like kinases [ Angiogenesis, 2024, 10.1007/s10456-024-09906-y] PubMed: 38403816
ELK3 destabilization by speckle-type POZ protein suppresses prostate cancer progression and docetaxel resistance [ Cell Death Dis, 2024, 15(4):274] PubMed: 38632244
The role of Pim-1 kinases in inflammatory signaling pathways [ Inflamm Res, 2024, 10.1007/s00011-024-01924-2] PubMed: 39079978
CDK9 inhibition induces epigenetic reprogramming revealing strategies to circumvent resistance in lymphoma [ Mol Cancer, 2023, 22(1):64] PubMed: 36998071
A novel IRAK4/PIM1 inhibitor ameliorates rheumatoid arthritis and lymphoid malignancy by blocking the TLR/MYD88-mediated NF-κB pathway [ Acta Pharm Sin B, 2023, 13(3):1093-1109] PubMed: 36970199
Nuclear transport surveillance of p53 by nuclear pores in glioblastoma [ Cell Rep, 2023, S2211-1247(23)00893-8] PubMed: 37552992
Targeting macrophagic PIM-1 alleviates osteoarthritis by inhibiting NLRP3 inflammasome activation via suppressing mitochondrial ROS/Cl- efflux signaling pathway [ J Transl Med, 2023, 21(1):452] PubMed: 37422640
Pivotal role of PIM2 kinase in plasmablast generation and plasma cell survival, opening new treatment options in myeloma [ Blood, 2022, blood.2021014011] PubMed: 35108359
Targeting PIM2 by JP11646 results in significant antitumor effects in solid tumors [ Int J Oncol, 2022, 61(4)114] PubMed: 35920189
Suppressive neutrophils require PIM1 for metabolic fitness and survival during chronic viral infection [ Cell Rep, 2021, 35(8):109160] PubMed: 34038722

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.