Powder: -20°C for 3 years | In solvent: -80°C for 1 year
I-BET567, a potent pan-BET inhibitor with oral activity, demonstrates pIC50 values of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. This compound has exhibited efficacy in mouse models of oncology and inflammation [1].
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 242.00 | |
5 mg | In stock | $ 592.00 | |
10 mg | In stock | $ 859.00 | |
25 mg | In stock | $ 1,280.00 | |
50 mg | In stock | $ 1,760.00 | |
100 mg | In stock | $ 2,370.00 |
Description | I-BET567, a potent pan-BET inhibitor with oral activity, demonstrates pIC50 values of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. This compound has exhibited efficacy in mouse models of oncology and inflammation [1]. |
In vitro | I-BET567 (compound 27) (72 hours; 1.5 nM-30 μM) significantly inhibits in vitro proliferation of the NMC cell line 11060, exhibiting a gpIC 50 of 6.2 (0.63 μM) [1]. This effect was observed in a Cell Viability Assay [1] conducted on NMC line 11060 cells, with a treatment concentration range of 1.5 nM-30 μM over 72 hours, resulting in markedly reduced cell growth. |
In vivo | I-BET567 (compound 27), administered orally at doses of 3, 10, and 30 mg/kg daily for 20 days, significantly reduced tumor growth in a NMC 11060 xenograft mouse model compared to vehicle controls at dosages of 10 and 30 mg/kg. Pharmacokinetic profiling of I-BET567, following both intravenous infusion and oral administration, was conducted in male Wistar Han rats and beagle dogs, revealing distinct pharmacokinetic parameters across species, doses, and administration routes. Notably, the oral bioavailability in rats and dogs was high, with values reaching 99% and 98%, respectively. This study elucidates the effectiveness of I-BET567 in tumor suppression and provides comprehensive pharmacokinetic data, including clearance rates, volume of distribution, and half-life across two species, which could inform future research and development efforts involving this compound. |
Molecular Weight | 359.81 |
Formula | C17H18ClN5O2 |
CAS No. | 1887237-54-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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I-BET567 1887237-54-8 I BET567 IBET567 I-BET-567 I-BET 567 inhibitor inhibit