AZD-1208 Chemical Properties

Melting point:

>220°C (dec.)

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)

form 

Solid

color 

Off-White to Pale Yellow

AZD-1208 Usage And Synthesis

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].

target

Pim1

IC 50

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

storage

Store at -20°C

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.

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