Name | AZD1208 |
Synonyms | CS-794 AZD1208 AZD-1208 AZD 1208 (R,Z)-5-((2-(3-aminopiperidin-1-yl)biphenyl-3-yl)methylene)thiazolidine-2,4-dione (R,Z)-5-((2-(3-aMinopiperidin-1-yl)-[1,1'-biphenyl]-3-yl)Methylene)thiazolidine-2,4-dione (5Z)-5-[[2-[(3R)-3-aMino-1-piperidinyl][1,1'-biphenyl]-3-yl]Methylene]-2,4-thiazolidinedione (5Z)-5-[[2-[(3R)-3-Amino-1-piperidinyl][1,1'-biphenyl]-3-yl]methylene]-2,4-thiazolidinedione AZD1208 |
CAS | 1204144-28-4 |
Molecular Formula | C21H21N3O2S |
Molar Mass | 379.48 |
Density | 1.307±0.06 g/cm3(Predicted) |
Melting Point | >220°C (dec.) |
Solubility | DMSO (Slightly) |
Appearance | Solid |
Color | Off-White to Pale Yellow |
pKa | 7.39±0.20(Predicted) |
Storage Condition | Hygroscopic, -20°C Freezer, Under inert atmosphere |
In vitro study | AZD1208 is an orally available, potent, highly selective Pim inhibitor that effectively inhibits three subtypes. AZD1208 inhibits the growth and sensitivity of several AML cell lines corresponding to Pim-1 expression levels, STAT5 activation and protein tyrosine kinase mutations. AZD1208 caused cell cycle arrest and apoptosis of MOLM-1 cells in culture. This was accompanied by a dose-dependent decrease in the phosphorylation of BAD,4EBP1 and p70S6K. In addition, AZD1208 effectively inhibited colony growth of AML cells in primary bone marrow aspirate and down-regulated phosphorylation of Pim targets. AZD1208 is an orally available, potent and highly selective Pim inhibitor that effectively inhibits three subtypes. AZD1208 inhibits the growth and sensitivity of several AML cell lines corresponding to Pim-1 expression levels, STAT5 activation and protein tyrosine kinase mutations. AZD1208 caused cell cycle arrest and apoptosis of MOLM-1 cells in culture. This was accompanied by a dose-dependent decrease in the phosphorylation of BAD,4EBP1 and p70S6K. In addition, AZD1208 effectively inhibited colony growth of AML cells in primary bone marrow aspirate and down-regulated phosphorylation of Pim targets. |
In vivo study | AZD1208 inhibited the growth of MOLM-16 and KG-1a xenograft tumors in vivo in proportion to the dose. AZD1208 inhibited the growth of MOLM-16 and KG-1a xenograft tumors in vivo in proportion to the dose. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.635 ml | 13.176 ml | 26.352 ml |
5 mM | 0.527 ml | 2.635 ml | 5.27 ml |
10 mM | 0.264 ml | 1.318 ml | 2.635 ml |
5 mM | 0.053 ml | 0.264 ml | 0.527 ml |