[CAS NO. 1613710-01-2]  ARN-3236

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PRODUCTS SPECIFICATIONS [1613710-01-2]

Catalog
HY-120856
Brand
MCE
CAS
1613710-01-2

DESCRIPTION [1613710-01-2]

Overview

MDLMFCD31813721
Molecular Weight336.41
Molecular FormulaC19H16N2O2S
SMILESCOC1=CC=C(C2=CNC3=NC=CC(C4=CSC=C4)=C32)C(OC)=C1

For research use only. We do not sell to patients.


Summary

ARN-3236 is an oral active and selective inhibitor of salt-inducible kinase 2 (SIK2) , with IC 50 s of <1 nM, 21.63 nM and 6.63 nM for SIK2 , SIK1 and SIK3 , respectively. Has anti-cancer activity [1] [2] .


IC50 & Target

SIK2

<1 nM (IC 50 )

SIK1

21.63 nM (IC 50 )

SIK3

6.63 nM (IC 50 )


In Vitro

ARN-3236 inhibits SIK2 activity with an IC 50 <1 nM [2] .
ARN-3236 inhibits cell growth and increases NSC 125973 sensitivity in ovarian cancer cells [2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay [2]

Cell Line: HEY and A2780 human ovarian cancer cell lines.
Concentration: 0-10 μM.
Incubation Time: 24 hours.
Result: Inhibited SIK2 activity with an IC 50 <1 nM.

In Vivo

ARN-3236 (60 mg/kg, orally) sensitizes ovarian cancer to NSC 125973 in vivo [2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 297.26 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.17 mg/mL (6.45 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.17 mg/mL (6.45 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.17 mg/mL (6.45 mM); Clear solution

* All of the co-solvents are available by MCE.