| Identification | Back Directory | [Name]
2,4-Thiazolidinedione, 5-[[2-[(3R)-3-amino-1-piperidinyl]-3-(1-methylethoxy)phenyl]methylene]-, (5Z)- | [CAS]
1204181-93-0 | [Synonyms]
AZD-1897
2,4-Thiazolidinedione, 5-[[2-[(3R)-3-amino-1-piperidinyl]-3-(1-methylethoxy)phenyl]methylene]-, (5Z)- | [Molecular Formula]
C18H23N3O3S | [MOL File]
1204181-93-0.mol | [Molecular Weight]
361.46 |
| Hazard Information | Back Directory | [Uses]
AZD1897 is a PIM1, PIM2, and PIM3 inhibitor with IC50 values of less than 3 nM for these three PIM kinases. AZD1897 exhibits anticancer activity and synergistically inhibits the activity of acute myeloid leukemia (AML) cells in combination with Capivasertib (HY-15431). This synergistic inhibitory effect is achieved through the inhibition of the mTOR and MCL1 pathways[1][2]. | [IC 50]
PIM1: <3 nM (IC50); PIM2: <3 nM (IC50); PIM3: <3 nM (IC50) | [References]
[1] Dakin LA, et al. 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. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4599-604. DOI:10.1016/j.bmcl.2012.05.098
[2] Meja K, et al. PIM and AKT kinase inhibitors show synergistic cytotoxicity in acute myeloid leukaemia that is associated with convergence on mTOR and MCL1 pathways. Br J Haematol. 2014 Oct;167(1):69-79. DOI:10.1111/bjh.13013 |
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