| Identification | Back Directory | [Name]
ARN-3236 | [CAS]
1613710-01-2 | [Synonyms]
ARN-3236
ARN-3236; ARN 3236; ARN3236
3-(2,4-Dimethoxyphenyl)-4-(3-thienyl)-1H-pyrrolo[2,3-b]pyridine
1H-Pyrrolo[2,3-b]pyridine, 3-(2,4-dimethoxyphenyl)-4-(3-thienyl)-
3-(2,4-DIMETHOXYPHENYL)-4-(THIOPHEN-3-YL)-1H-PYRROLO[2,3-B]PYRIDINE | [Molecular Formula]
C19H16N2O2S | [MDL Number]
MFCD31813721 | [MOL File]
1613710-01-2.mol | [Molecular Weight]
336.41 |
| Chemical Properties | Back Directory | [density ]
1.278±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:65.67(Max Conc. mg/mL);195.21(Max Conc. mM)
Ethanol:2.0(Max Conc. mg/mL);5.95(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);89.18(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:4):0.2(Max Conc. mg/mL);0.59(Max Conc. mM) | [form ]
A crystalline solid | [pka]
13.33±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Biological Activity]
ARN-3236 is an orally activeATP-competitiveSIK2-selective salt-inducible kinase inhibitor (IC50 = 21.63 nM/SIK1<1 nM/SIK26.63 nM/SIK3) th at suppresses cellular SIK2 activity (by 58% at 1 μM; SKOv3-SIK2 cells48 h) with high selectivity over >456 kinases. ARN-3236 effectively suppresses SIK2-dependent growth of ovarian cancer cultures (IC50 = 0.8-2.6 μM in 10 lines72 h) and in murine xenograft models in vivo (3060100 mg/kg/day p.o.). In additionARN-3236 sensitizes ovarian cancer cells to paclitaxel in vitro and in vivo. ARN-3236 completes the SIK1-selective HG-9-91-01 (SIK1/2/3 IC50 = 0.6/6.6/9.6 nM) in probing SIKs-mediated cellular signaling events. | [storage]
Store at -20°C |
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