I-BET567 is a potent and orally active inhibitor of pan-BET candidate with pIC 50 s 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.
性状
Solid
IC50 & Target[1][2]
BRD4 (BD1) 6.9 (pIC50) BRD2 7.2 (pIC
体外研究(In Vitro)
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). has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay
体内研究(In Vivo)
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.
Assessment of Pharmacokinetics (PK) profile of I-BET567 following intravenous infusion and oral administration in male wistar han rat and beagle dog.
species
dose iv/po (mg/kg)
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献
[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].
溶解度数据
In Vitro: DMSO : 100 mg/mL (277.92 mM; Need ultrasonic)配制储备液