AZD 1208

Biological Activity

AZD 1208 is a potent pan Pim kinase inhibitor (IC₅₀ values are 0.4, 1.9 and 5.0 nM for Pim-1, 3 and 2, respectively). Exhibits >43-fold higher affinity for Pim kinases over a range of other kinases. Induces cell cycle arrest and apoptosis in AML cell lines in vitro and inhibits growth of tumor xenografts in vivo. AZD 1208 downmodulates the expression of Mayaro virus (MAYV) structural protein E1 and non-structural protein 1 (nsP1), and it reduces MAYV replication in a dose-dependent manner in HeLa or HDFs cells. Chemosensitizer.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. AZD1208, a potent and selective pan-Pim kinase inhibitor, demonstrates efficacy in preclinical models of acute myeloid leukemia.
   Keeton et al.
   Blood, 2014;123:905
2. PIM1 kinase regulates cell death, tumor growth and chemotherapy response in triple-negative breast cancer.
   Brasó-Maristany et al.
   Nat.Med., 2016;22:1303
3. Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases.
   Dakin et al.
   Bioorg.Med.Chem.Lett., 2012;22:4599

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