Biological Activity
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, as well as sensitizing tumors to chemotherapy.
Technical Data
| M. Wt | 379.48 |
| Formula | C21H21N3O2S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1204144-28-4 |
| PubChem ID | 58423153 |
| InChI Key | MCUJKPPARUPFJM-UWCCDQBKSA-N |
| Smiles | N[C@@H]1CCCN(C2=C(C3=CC=CC=C3)C=CC=C2/C=C4SC(NC4=O)=O)C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 7.59 | 20mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 379.48. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.64 mL | 13.18 mL | 26.35 mL |
| 5 mM | 0.53 mL | 2.64 mL | 5.27 mL |
| 10 mM | 0.26 mL | 1.32 mL | 2.64 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.53 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Keeton et al (2014) AZD1208, a potent and selective pan-Pim kinase inhibitor, demonstrates efficacy in preclinical models of acute myeloid leukemia. Blood 123 905 PMID: 24363397
Brasó-Maristany et al (2016) PIM1 kinase regulates cell death, tumor growth and chemotherapy response in triple-negative breast cancer. Nat.Med. 22 1303 PMID: 27775704
Dakin et al (2012) 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. 22 4599 PMID: 22727640
Keywords: AZD 1208, supplier, AZD1208, pan, Pim, kinase, 1, 2, 3, potent, active, in, vivo, anticancer, inhibitors, inhibits, Pim, Kinase, Pim, Kinase, Tocris Bioscience
