[CAS NO. 1311367-27-7] BIX02565
PRODUCTS SPECIFICATIONS [1311367-27-7]
DESCRIPTION [1311367-27-7]
Overview
| MDL | MFCD25976796 |
|---|---|
| Molecular Weight | 458.56 |
| Molecular Formula | C26H30N6O2 |
| SMILES | O=C(C1=CC2=C(C=C1)C=C3N2[C@H](C)CCNC3=O)NC4=NC5=CC=CC=C5N4CCCN(C)C |
4 Publications Citing Use of MCE
Summary
BIX 02565 is a potent ribosomal S6 kinase 2 ( RSK2 ) inhibitor with IC 50 of 1.1 nM.
IC50 & Target
IC50: 1.1 nM (RSK2) [1]
In Vitro
BIX 02565, a potent RSK2 inhibitor (IC 50 =1.1 nM) targets for the treatment of heart failure secondary to myocardial infarction through indirect NHE inhibition [1] . BIX 02565, a second Rsk inhibitor, protects enzyme active sites from reaction with biotinylated nucleotide acyl phosphates [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
In telemetry-instrumented rats, BIX 02565 (30, 100, and 300 mg/kg p.o. QD for 4 days) elicits concentration-dependent decreases in MAP after each dose (to -39±4 mm Hg on day 4 at T max ). BIX 02565 produces concentration-dependent relaxation ex vivo in the phenylephrine-constricted rat aortic ring at concentrations above 0.03 μM with a calculated EC 50 of 3.1 μM. Subsequently, BIX 02565 is infused in the anesthetized rat in a low-dose (0.1, 0.3, and 1.0 mg/kg per 20 min) and high-dose (1.0, 3.0, and 10.0 mg/kg per 20 min) series of continuous infusions to test the effect of compound on hemodynamics in vivo [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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
DMSO : 20.75 mg/mL ( 45.25 mM ; Need ultrasonic and warming)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1807 mL | 10.9037 mL | 21.8074 mL |
| 5 mM | 0.4361 mL | 2.1807 mL | 4.3615 mL |
| 10 mM | 0.2181 mL | 1.0904 mL | 2.1807 mL |
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Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 1.67 mg/mL (3.64 mM); Clear solution
References
- [1] Fryer RM, et al. Mitigation of off-target adrenergic binding and effects on cardiovascular function in the discovery of novel ribosomal S6 kinase 2 inhibitors. Journal of Pharmacology and Experimental Therapeutics (2012), 340(3), 492-500.
- [2] Edgar AJ, et al. A combination of SILAC and nucleotide acyl phosphate labelling reveals unexpected targets of the Rsk inhibitor BI-D1870. Biosci Rep. 2013 Dec 17.