SML3802

ARN-3236

≥98% (HPLC)

• Synonym(s): 3-(2,4-Dimethoxyphenyl)-4-(3-thienyl)-1H-pyrrolo[2,3-b]pyridine, 3-(2,4-Dimethoxyphenyl)-4-(thiophen-3-yl)-1H-pyrrolo[2,3-b]pyridin, ARN 3236, ARN3236
• Empirical Formula (Hill Notation): C₁₉H₁₆N₂O₂S
• CAS Number: 1613710-01-2
• Molecular Weight: 336.41
• UNSPSC Code: 12352200
• NACRES: NA.21
• MDL number: MFCD31813721
• Assay: ≥98% (HPLC)
• Form: powder

Properties

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: 2-8°C
• SMILES string: [s]1cc(cc1)c2c3c([nH]cc3c4c(cc(cc4)OC)OC)ncc2
• InChI: 1S/C19H16N2O2S/c1-22-13-3-4-15(17(9-13)23-2)16-10-21-19-18(16)14(5-7-20-19)12-6-8-24-11-12/h3-11H,1-2H3,(H,20,21)
• InChI key: WEHOIIGXTMKVRG-UHFFFAOYSA-N

Description

Biochem/physiol Actions

ARN-3236 is an orally active, ATP-competitive, SIK2-selective salt-inducible kinase inhibitor (IC50 = 21.63 nM/SIK1, <1 nM/SIK2, 6.63 nM/SIK3) that suppresses cellular SIK2 activity (by 58% at 1 μM; SKOv3-SIK2 cells, 48 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 lines, 72 h) and in murine xenograft models in vivo (30, 60, 100 mg/kg/day p.o.). In addition, ARN-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.

Orally active, ATP-competitive, highly potent and selective SIK2 inhibitor with anti-ovarian cancer efficacy in vitro and in vivo.

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable