I-BET282 (C09-1139-931)

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 VitroI-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 VivoI-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.Form:Solid. Specifications and Purity: 99%. Molecular Formula: C25H30N4O4. Molecular Weight: 450.53. PubChem CID: 71258968. Isomeric SMILES: CC1=C(C(=NO1)C)C2=C(C=C3C(=C2)N=CC4=C3N(C(=N4)C5CCOCC5)[C@H](C)COC)OC.