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AZD-1208 is a potent and selective pan-Pim kinase inhibitor which demonstrates efficacy in preclinical models of acute myeloid leukemia. AZD1208 inhibited the growth of 5 of 14 acute myeloid leukemia (AML) cell lines tested, and sensitivity correlates with Pim-1 expression and STAT5 activation. AZD1208 causes cell cycle arrest and apoptosis in MOLM-16 cells, accompanied by a dose-dependent reduction in phosphorylation of Bcl-2 antagonist of cell death, 4EBP1, p70S6K, and S6, as well as increases in cleaved caspase 3 and p27.AZD1208 inhibits the growth of MOLM-16 and KG-1a xenograft tumors in vivo with a clear pharmacodynamic-pharmacokinetic relationship. AZD1208 also potently inhibits colony growth and Pim signaling substrates in primary AML cells from bone marrow that are Flt3 wild-type or Flt3 internal tandem duplication mutant.AZD1208 inhibited tumorigenesis in tissue recombinants, Myc-CaP, and human PC xenograft models.AZD1208 suppressed multiple protumorigenic pathways, including the MYC gene program.
Invest New Drugs. 2025 Mar 17;43(2):301-310.
Evaluation of the anti-leukemia activity and underlying mechanisms of the novel perinucleolar compartment inhibitor CTI-2 in acute myeloid leukemia
AZD-1208 purchased from AbMole
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Source | Oncotarget (2017). Figure 1. AZD-1208 |
| Method | Cell counting Kit-8 assay | |
| Cell Lines | MV4-11 cells | |
| Concentrations | 1 μM | |
| Incubation Time | 48 h | |
| Results | As shown in Figure 1J, AZD1208 and GDC-0941 synergistically reduced viable cell numbers of MV4-11, as judged by combination index (CI) values obtained by the method of Chuo and Talalay being less than 1 at all the concentrations examined. |
| Cell Experiment | |
|---|---|
| Cell lines | EOL-1, KG-1a, Kasumi-3, MV4-11, and MOLM-16 cells |
| Preparation method | For proliferation assays, cells were plated at 5,000 to 20,000 cells per well in 96 well plates overnight before treatment for 72 hours with serially diluted compound or vehicle DMSO. Cell viability was measured after the addition of 10 μL Alamar Blue (Invitrogen) for 4 hours at 37˚C. The GI50 was determined by calculating growth at each dose relative to vehicle treated cells and cell viability at the time of treatment. |
| Concentrations | 0~11 μM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | Female CB17 SCID mice bearing MOLM-16 cells or KG-1a cells xenografts model |
| Formulation | 0.5% hydroxypropyl methylcellulose |
| Dosages | 3, 10 and 30mg/kg daily for 14 days |
| Administration | oral gavage |
| Molecular Weight | 379.48 |
| Formula | C21H21N3O2S |
| CAS Number | 1204144-28-4 |
| Solubility (25°C) | DMSO >28 mg/ml |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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| SMI-4a
SMI-4a is a potent inhibitor of Pim1 with IC50 of 17 nM, modest potent to Pim-2, does not significantly inhibit other serine/threonine- or tyrosine-kinases. |
| CX-6258
CX-6258 is a potent, orally efficacious Pim 1/2/3 kinase(IC50=5 nM/25 nM/16 nM) inhibitor with excellent biochemical potency and kinase selectivity. |
| TCS PIM-1 1
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| Hispidulin
Hispidulin is a natural flavonoid with a wide range of biological activities. Hispidulin is an inhibitor of PIM-1 with IC50 value of 2.71 μM. Hispidulin induces apoptosis through mitochondrial dysfunction and inhibition of P13k/Akt signalling pathway in HepG2 cancer cells. |
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