Table 1 Novel Pim-Inhibitors in hematologic malignancies

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