ARN-3236
- CAS No.
- 1613710-01-2
- Chemical Name:
- ARN-3236
- Synonyms
- ARN-3236;ARN-3236, 10 mM in DMSO;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;inhibit,ARN3236,Salt-inducible Kinase (SIK),ARN-3236,ARN 3236,Inhibitor
- CBNumber:
- CB23339851
- Molecular Formula:
- C19H16N2O2S
- Molecular Weight:
- 336.41
- MDL Number:
- MFCD31813721
- MOL File:
- 1613710-01-2.mol
| 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 |
| UNSPSC Code | 12352200 |
| NACRES | NA.21 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302-H315-H319-H335 | |||||||||
| Precautionary statements | P261-P305+P351+P338 | |||||||||
| NFPA 704 |
|
ARN-3236 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| ChemScene | CS-0079380 | ARN-3236 99.60% | 1613710-01-2 | 5mg | $150 | 2021-12-16 | Buy |
| ChemScene | CS-0079380 | ARN-3236 99.60% | 1613710-01-2 | 10mg | $250 | 2021-12-16 | Buy |
| ChemScene | CS-0079380 | ARN-3236 99.60% | 1613710-01-2 | 2mg | $100 | 2021-12-16 | Buy |
| Axon Medchem | Axon3041 | ARN3236 98% | 1613710-01-2 | 5mg | $104.5 | 2021-12-16 | Buy |
| ChemScene | CS-0079380 | ARN-3236 99.60% | 1613710-01-2 | 50mg | $550 | 2021-12-16 | Buy |
ARN-3236 Chemical Properties,Uses,Production
Uses
ARN-3236 is an oral active and selective inhibitor of salt-inducible kinase 2 (SIK2), with IC50s of <1 nM, 21.63 nM and 6.63 nM for SIK2, SIK1 and SIK3, respectively. Has anti-cancer activity[1][2].
Biological Activity
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) th at 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.
in vivo
ARN-3236 (60 mg/kg, orally) sensitizes ovarian cancer to NSC 125973 in vivo[2].
| Animal Model: | SKOv3ip-bearing mice and OVCAR8-bearing mice[2]. |
| Dosage: | 60 mg/kg. |
| Administration: | Orally once daily for 3 weeks (SKOv3ip-bearing mice) and 4 weeks (OVCAR8-bearing mice). |
| Result: | Sensitized ovarian cancer to NSC 125973. |
IC 50
SIK2: <1 nM (IC50); SIK1: 21.63 nM (IC50); SIK3: 6.63 nM (IC50)
storage
Store at -20°C
References
[1] Lombardi MS, et al. SIK inhibition in human myeloid cells modulates TLR and IL-1R signaling and induces an anti-inflammatory phenotype. J Leukoc Biol. 2016 May;99(5):711-21. DOI:10.1189/jlb.2A0715-307R
[2] Zhou J, et al. A Novel Compound ARN-3236 Inhibits Salt-Inducible Kinase 2 and Sensitizes Ovarian Cancer Cell Lines and Xenografts. Clin Cancer Res. 2017 Apr 15;23(8):1945-1954. DOI:10.1158/1078-0432.CCR-16-1562
ARN-3236 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| Biochempartner | 0086-13720134139 | candy@biochempartner.com | CHINA | 965 | 58 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19552 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32268 | 58 |
| Career Henan Chemica Co | +86-0371-86658258 +8613203830695 | laboratory@coreychem.com | China | 30230 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6312 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10473 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | sales@chemhifuture.com | China | 3135 | 58 |
| TargetMol Chemicals Inc. | support@targetmol.com | United States | 38663 | 58 |
