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Featured Inhibitors for OctoberBOC Sciences
Quizartinib
• Quizartinib is an orally available small
molecule with potential antineoplastic activity.
Class III receptor tyrosine kinase inhibitor
AC220 selectively inhibits class III receptor
tyrosine kinases, including FMS-related
tyrosine kinase 3 (FLT3/STK1), colonystimulating factor 1 receptor (CSF1R/FMS),
stem cell factor receptor (SCFR/KIT), and
platelet derived growth factor receptors
(PDGFRs), resulting in inhibition of ligandindependent leukemic cell proliferation and
apoptosis.
PIK-75
• PIK-75 was developed as part of a PI 3-kinase
drug discovery program. PIK75 attenuates
insulin stimulation of Akt/PKB in a range of
cell types at 100 nM. The compound has been
reported to block growth of a range of cell
lines with an IC50 value in the region of 50
nM. In vivo studies have shown that PIK-75,
administered at 50 mg/kg, inhibited the
growth of HeLa cell xenografts in mice models.
WAY-252623
• WAY-252623 (LXR-623) is a highly selective
and orally bioavailable synthetic modulator of
LXR, which can reduces total serum
cholesterol and LDL cholesterol and inhibits
lesion growth in models of atherosclerosis.
IC50 values= 24 and 179 nM (for LXRβ and
LXRα, respectively)
GW3965
GW3965 is a potent, selective LXR agonist for
hLXRα and hLXRβ. When screened against a
panel of nuclear receptors, it cross-reacted
with only the pregnane X receptor (PXR). In
Vitro: Recruit the steroid receptor coactivator
1 to human LXRα with EC50 of 125 nM in a
cell-free ligand-sensing assay
Cyt387
• Cyt387, also called Momelotinib, under the
IUPAC name N-(cyanomethyl)-4-(2-((4-(4morpholinyl)phenyl)amino)-4pyrimidinyl)benzamide, is an ATP competitive
inhibitor of JAK1 (IC50 = 11 nM) and JAK2
(IC50 = 18 nM) with potential antineoplastic
activity, which may result result in the
induction of apoptosis and a reduction of
tumor cell proliferation in JAK1/2-expressing
tumor cells.