I-BET282 - 10mM in DMSO, high purity , CAS No.1422554-34-4(DMSO)

Item Number

I655139

• Specifications & Purity: 10mM in DMSO
• Storage Temp: Store at -80°C
• Shipped In: Dry ice

Product Description

I-BET282 is a pan-inhibitor of all eight BET bromodomains , and selectivity over other representative bromodomain-containing proteins. I-BET282 shows pIC 50 s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD).

In Vitro

I-BET282 has a weak inhibition of the hERG potassium ion channel (pIC 50 4.4-5.1 in a variety of assay formats). I-BET282 shows a low potential to inhibit CYP proteins in vitro, with no evidence of time-dependent inhibition of 2D6 or 3A4. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

I-BET282 (Male CD1 Mice; 3 mg/kg-p.o.; 1 mg/kg-i.v.) treatment shows the Cl b , LBF, Vss, t 1/2 (i.v.), and F values of 23 mL/min/kg, 19%, 1.9 L/kg, and 51%, respectively. I-BET282 (Male Wistar Han Rats; 1 mg/kg; p.o.) treatment shows the AUC 0-t , C max and T max values of 467 ng h/mL, 125 ng/mL, and 1 hour, respectively . MCE has not independently confirmed the accuracy of these methods. They are for reference only.