1204144-28-4

Basic information

• Product Name: AZD-1208
• Synonyms: AZD 1208;AZD1208;AZD-1208;(5Z)-5-[[2-[(3R)-3-aMino-1-piperidinyl][1,1'-biphenyl]-3-yl]Methylene]-2,4-thiazolidinedione;(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 AZD1208;(R,Z)-5-((2-(3-aminopiperidin-1-yl)biphenyl-3-yl)methylene)thiazolidine-2,4-dione;AZD1208 >=95%
• CAS NO: 1204144-28-4
• Molecular Formula: C21H21N3O2S
• Molecular Weight: 379.47534
• Product Categories: JAK/STAT;Inhibitors;JAK;STAT
• Mol File: 1204144-28-4.mol
• Article Data: 1

Chemical Properties

• Appearance: /
• Density: 1.307±0.06 g/cm3(Predicted)
• Storage Temp.: Hygroscopic, -20°C Freezer, Under inert atmosphere
• Solubility: DMSO (Slightly)
• PKA: 7.39±0.20(Predicted)
• CAS DataBase Reference: AZD-1208(CAS DataBase Reference)
• NIST Chemistry Reference: AZD-1208(1204144-28-4)
• EPA Substance Registry System: AZD-1208(1204144-28-4)

Safety Data

• Hazardous Substances Data: 1204144-28-4(Hazardous Substances Data)

Usage

Uses

AZD1208 is a potent, and orally available Pim kinase inhibitor.

Biological Activity

upregulation of pim kinases has been observed in several types of leukemias and lymphomas. pim-1, -2, and -3 promote cell proliferation and survival downstream of cytokine and growth factor signaling pathways. azd1208 is a potent, highly selective, and orally available pim kinase inhibitor.

in vitro

azd1208 inhibited the growth of 5 of 14 acute myeloid leukemia (aml) cell lines tested. in molm-16 cells, azd1208 also causes cell cycle arrest and apoptosis, accompanied by a dose-dependent reduction in phosphorylation of bcl-2 antagonist of cell death [1].

in vivo

azd1208 inhibits the growth of kg-1a and molm-16 xenograft tumors in vivo with a clear pk/pd relationship. treatment with 10 mg/kg or 30 mg/kg of azd1208 led to an 89% tumor growth inhibition or slight regression, respectively [1].

IC 50

0.4 nm for pim-1, 5.0 nm for pim-2, and 1.9 nm for pim-3

references

[1] keeton ek, mceachern k, dillman ks, palakurthi s, cao y, grondine mr, kaur s, wang s, chen y, wu a, shen m, gibbons fd, lamb ml, zheng x, stone rm, deangelo dj, platanias lc, dakin la, chen h, lyne pd, huszar d. azd1208, a potent and selective pan-pim kinase inhibitor, demonstrates efficacy in preclinical models of acute myeloid leukemia. blood. 2014;123(6):905-13.

Relevant articles and documents

CHEMICAL COMPOUNDS 251

The invention relates to chemical compounds of formula (I), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of PIM-1 and/or PIM-2, and/or PIM-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of PIM kinase related conditions and diseases, preferably cancer.