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AZD 1208

Cat. No. 6310 1 Citation Submit a Review Datasheet / COA / SDS
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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 (1)
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for AZD 1208

AZD 1208 is a 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. AZD 1208 downmodulates the expression of Mayaro virus (MAYV) structural protein E1 and non-structural protein 1 (nsP1), and it reduces MAYV replication in a dose-dependent manner in HeLa or HDFs cells. Chemosensitizer.

Technical Data for AZD 1208

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 for AZD 1208

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 7.59 20 with gentle warming

Preparing Stock Solutions for AZD 1208

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.

Select a batch to recalculate based on the batch molecular weight:
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 for AZD 1208

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

Salazar et al (2022) Targeting host PIM protein kinases reduces Mayaro virus replication. Viruses 14 422 PMID: 35216015

If you know of a relevant reference for AZD 1208, please let us know.

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1 Citation for AZD 1208

Citations are publications that use Tocris products. Selected citations for AZD 1208 include:

Salazar et al (2022) Targeting host PIM protein kinases reduces Mayaro virus replication. Viruses 14 422 PMID: 35216015

Do you know of a great paper that uses AZD 1208 from Tocris? Please let us know.

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Literature in this Area

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