[CAS NO. 1613710-01-2] ARN-3236
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PRODUCTS SPECIFICATIONS [1613710-01-2]
Catalog
SLK-S8543
Brand
Selleck
CAS
1613710-01-2
DESCRIPTION [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
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.
Targets
In vitro
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.
References
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