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AZD 1208

Cat. No. 6310 Submit a Review Datasheet / COA / SDS
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Cat.No. 6310 - AZD 1208 | C21H21N3O2S | CAS No. 1204144-28-4
Description: Potent pan Pim kinase inhibitor
Chemical Name: (5Z)-5-[[2-[(3R)-3-Amino-1-piperidinyl][1,1'-biphenyl]-3-yl]methylene]-2,4-thiazolidinedione
Purity: ≥98% (HPLC)
Datasheet
Citations
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Literature
Biological Activity Technical Data Solubility Calculators Datasheets References

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 the degree 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

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