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. Form:Solid
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I-BET282
CAS number：1422554-34-4 molecular formula：C25H30N4O4
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 1422554-34-4 | molecular formula | C25H30N4O4 |
| molecular weight | 450.53 g/mol | Exact mass | ≥99% |
| PSA | 84.400 Ų | logp | 3.200 |
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