[CAS NO. 1665195-94-7] BAZ2-ICR
PRODUCTS SPECIFICATIONS [1665195-94-7]
DESCRIPTION [1665195-94-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 357.41 |
| Molecular Formula | C20H19N7 |
| SMILES | N#CC1=CC=C(C2=C(C3=CN(C)N=C3)N=CN2CCC4=CN(C)N=C4)C=C1 |
Summary
BAZ2-ICR is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC 50 s of 130 nM and 180 nM, and K d s of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains. BAZ2-ICR is an epigenetic chemical probe [1] .
IC50 & Target
IC50: 130 nM (BAZ2A) and 180 nM (BAZ2B); Kd: 109 nM (BAZ2A) and 170 nM (BAZ2A) [1]
In Vitro
To investigate whether BAZ2-ICR (Compound 13) can displace BAZ2 bromodomains from chromatin in living cells, a fluorescence recovery after photobleaching (FRAP) assay utilizing GFP-tagged BAZ2A full length protein transfected into human osteosarcoma cells (U2OS) are tested. 1 μM BAZ2-ICR reduces the recovery time of the wild-type (wt) construct to a level similar to the dominant negative mutant, confirming that BAZ2-ICR inhibits BAZ2A in cells [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
BAZ2-ICR (Compound 13) shows very high solubility (25 mM in D2O), a measured log D of 1.05, high stability in mouse microsomes, and permeation in the CaCo-2 model and thus a suitable profile for oral and intravenous gavage. BAZ2-ICR (5 mg/kg) shows 70% bioavailability and moderate clearance (∼50% of mouse liver blood flow) and volume of distribution [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
DMF : 20 mg/mL ( 55.96 mM ; Need ultrasonic and warming)
DMSO : 10 mg/mL ( 27.98 mM ; Need ultrasonic and warming)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.7979 mL | 13.9895 mL | 27.9791 mL |
| 5 mM | 0.5596 mL | 2.7979 mL | 5.5958 mL |
| 10 mM | 0.2798 mL | 1.3990 mL | 2.7979 mL |