AZD1208

AZD1208

Catalog Number:
L002368944APE
Mfr. No.:
APE-A3962
Price:
$223
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      • Overview
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          Background

          IC50: 0.4 nM for Pim-1, 5.0 nM for Pim-2, and 1.9 nM for Pim-3
          Upregulation of Pim kinases has been observed in several types of leukemias and lymphomas. Pim-1, -2, and -3 promote cell proliferation and survival downstream of cytokine and growth factor signaling pathways. AZD1208 is a potent, highly selective, and orally available Pim kinase inhibitor.
          In vitro: AZD1208 inhibited the growth of 5 of 14 acute myeloid leukemia (AML) cell lines tested. In MOLM-16 cells, AZD1208 also causes cell cycle arrest and apoptosis, accompanied by a dose-dependent reduction in phosphorylation of Bcl-2 antagonist of cell death [1].
          In vivo: AZD1208 inhibits the growth of KG-1a and MOLM-16 xenograft tumors in vivo with a clear PK/PD relationship. Treatment with 10 mg/kg or 30 mg/kg of AZD1208 led to an 89% tumor growth inhibition or slight regression, respectively [1].
          Clinical trials: AZD1208 is in Phase I trials evaluating the safety and tolerability profile and to determine the maximum tolerated dose (MTD). There are two ongoing trials where AZD1208 has been orally administered in AML and solid tumor (of all types) patients

      • Properties
        • Alternative Name
          AZD 1208;AZD-1208; (5E)-5-[[2-[(3R)-3-aminopiperidin-1-yl]-3-phenylphenyl]methylidene]-1,3-thiazolidine-2,4-dione
          CAS Number
          1204144-28-4
          Molecular Formula
          C21H21N3O2S
          Molecular Weight
          379.48
          Appearance
          A solid
          Purity
          99.58%
          Solubility
          insoluble in EtOH; insoluble in H2O; ≥18.95 mg/mL in DMSO
          Storage
          Store at -20°C

          * For Research Use Only

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