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Catalog:
SLK-S8543
Brand:
Selleck
CAS:
1613710-01-2
Overview
MDL
MFCD31813721
Molecular Weight
336.41
Molecular Formula
C19H16N2O2S
SMILES
COC1=CC=C(C2=CNC3=NC=CC(C4=CSC=C4)=C32)C(OC)=C1
For research use only.
Storage
3 years,-20°C,powder 1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
1 mg
5 mg
10 mg
1 mM
2.9726 mL
14.8628 mL
29.7256 mL
5 mM
0.5945 mL
2.9726 mL
5.9451 mL
10 mM
0.2973 mL
1.4863 mL
2.9726 mL
50 mM
0.0595 mL
0.2973 mL
0.5945 mL
Description
ARN-3236 is a potent, orally available and selective inhibitor of with IC50 of <1 nM, 21.63 nM and 6.63 nM for SIK2, SIK1 and SIK3, respectively. ARN-3236 induces in cancer cells.
SIK2 is overexpressed in approximately 30% of high grade serous ovarian cancers. ARN-3236 inhibits growth of 10 ovarian cancer cell lines at an IC50 of 0.8 to 2.6 μM, where the IC50 of ARN-3236 is inversely correlated with endogenous SIK2 expression (Pearson’s r = −0.642, P = 0.03). ARN-3236 enhances sensitivity to paclitaxel in 8 of 10 cell lines. In at least three cell lines a synergistic interaction is observed. ARN-3236 uncouples the centrosome from the nucleus in interphase, blocks centrosome separation in mitosis, causes prometaphase arrest and induces apoptotic cell death and tetraploidy. ARN-3236 also inhibits AKT phosphorylation and attenuates survivin expression.