AZD 1208
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. Chemosensitizer.
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(NC\4=O)=O)C1 |
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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 7.59 | 20 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 |
|---|---|---|---|
| 0.2 mM | 13.18 mL | 65.88 mL | 131.76 mL |
| 1 mM | 2.64 mL | 13.18 mL | 26.35 mL |
| 2 mM | 1.32 mL | 6.59 mL | 13.18 mL |
| 10 mM | 0.26 mL | 1.32 mL | 2.64 mL |
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References
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for AZD 1208, please let us know.
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Citations for AZD 1208
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Cancer Research Product Guide
A collection of over 750 products for cancer research, the guide includes research tools for the study of:
- Cancer Metabolism
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- Receptor Signaling
- Cell Cycle and DNA Damage Repair
- Angiogenesis
- Invasion and Metastasis
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A collection of over 400 products for kinase research, the listing includes inhibitors of:
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- PI-3 Kinase, Akt and mTOR
- MAPK Signaling
- Receptor Serine/Threonine Kinases
