产品
编 号：F747736
分子式：C17H18ClN5O2
分子量：359.81
分子式：C17H18ClN5O2
分子量：359.81
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
结构图
CAS No: 1887237-54-8
产品详情
生物活性：
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.
体内研究：
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 doga.speciesdose 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
dog1.0/38.1206.91.22.91.8980.41
a: 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.Animal Model:NMC 11060 xenograft mouse model (NOD/SCID mouse; bearing NMC 11060 cells)
Dosage:3, 10, and 30 mg/kg
Administration:p.o. (once daily for 20 days
Result:Led to a significant reduction in tumor growth compared to vehicle controls at both 10 and 30 mg/kg.
体外研究：
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).
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.
体内研究：
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 doga.speciesdose 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
dog1.0/38.1206.91.22.91.8980.41
a: 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.Animal Model:NMC 11060 xenograft mouse model (NOD/SCID mouse; bearing NMC 11060 cells)
Dosage:3, 10, and 30 mg/kg
Administration:p.o. (once daily for 20 days
Result:Led to a significant reduction in tumor growth compared to vehicle controls at both 10 and 30 mg/kg.
体外研究：
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).
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备