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. 2014 Dec 10;7:95. doi: 10.1186/s13045-014-0095-z

Table 1.

Novel Pim-Inhibitors in hematologic malignancies

Compound Class PIM inhibition selectivity Development Disease
SGI-1776 imadizaopyridazine IC50: 7 nM PIM1, 363 nM PIM2, 69 nM PIM3, 44 nM FLT-3 and 34 nM Haspin [107]. Failure in phase I clinical trials by cardiotoxicity Non-Hodgkin lymphoma
SMI4a benzylidene-thiazolidene-2,4-dione IC50: 21 nM PIM1, 100 nM PIM2 [113]. Preclinical Acute myeloid leukemia
Selective vs. 56 kinases [114].
LGB321 3-(S)-amino-piperidine pyridyl carboxamide IC50: 0.001 nM PIM1, 0.0021 nM PIM2, and 0.0008 nM PIM3 [106]. Recruiting patients for clinical trials Multiple myeloma
AZD1897 IC50: 3 nM PIM1,2 and 3 [115]. Preclinical Acute myeloid leukemia
SEL24-B58 Benzoimidazol IC50: 31 nM PIM1, 154 nM PIM2, 152 nM PIM3. Selective in a panel of 299 kinases with the exception of haspin, HIPK and CLK kinases [117]. Preclinical Leukemic monocyte lymphoma
AZD1208 thiazolidene IC50: Pim-1 0.4 nM, Pim-2 5.0 nM and Pim-3 1.9 nM [115]. Recruiting patients for clinical trials Acute myeloid leukemia