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 |