I-BET567 |
Catalog No.GC64297 |
I-BET567 is a potent and orally active inhibitor of pan-BET candidate with pIC50s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1887237-54-8
Sample solution is provided at 25 µL, 10mM.
I-BET567 is a potent and orally active inhibitor of pan-BET candidate with pIC50s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation[1].
I-BET567 (compound 27) (72 hours; 1.5 nM-30 μM) effectively inhibites the proliferation of human NMC cell line 11060 in vitro with a mean gpIC50 6.2 (0.63 μM)[1].
I-BET567 (compound 27) (3, 10, and 30 mg/kg; p.o.; once daily for 20 days) leads to a significant reduction in tumor growth compared with vehicle controls at both 10 and 30 mg/kg[1].Assessment of Pharmacokinetics (PK) profile of I-BET567 following intravenous infusion and oral administration in male wistar han rat and beagle doga[1]. species dose ivb/poc (mg/kg) CLb (mL/min/kg) CLb,u (mL/min/kg) CLrenal (mL/min/kg) Vss (L/kg) Vss,u (L/kg) t1/2 (h) Fpo (%) fub rat1.3/32510972.410.41.699d0.23 dog1.0/38.1206.91.22.91.8980.41a: Values are mean, n=3 unless otherwise stated. b: IV dose 1h infusion in DMSO and (10%, w/v) Kleptose HPB in saline (2%: 98% (v/v)). c: PO dose vehicle: 1%(w/v) methycellulose (400 cps) (aq). d: Mean n = 2.
[1]. Humphreys PG, et al. Design, Synthesis, and Characterization of I-BET567, a Pan-Bromodomain and Extra Terminal (BET) Bromodomain Oral Candidate [published online ahead of print, 2022 Jan 7].
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