产品
编 号：F747120
分子式：C30H29D3FN5O2
分子量：516.62
分子式：C30H29D3FN5O2
分子量：516.62
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规格
价格
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CAS No: 1800343-11-6
产品详情
生物活性：
BET-IN-12 is an orally avtive inhibitor of bromodomain and extra-terminal (BET) with an IC50 of 0.9 nM for BRD4.
体内研究：
BET-IN-12 (compound 15) is 100% oral bioavailability in mouse.BET-IN-12 (compound 15) impairs the growth of established PDX tumors (TGI = 88%) at MED = 2 mg/kg (AUC = 4800 nM?h).pharmacokinetic (PK) profile dose (iv/po, mg/kg)CLp ((mL/min)/kg)Vd (L/kg) half-life (ie, h)F (%) AUC (po, nM.h)
mouse1.0/3.04.21.43.410025000
rat1.0/5.0182.94.1746600
dog0.1/0.3135.87.673550
monkey0.1/0.34.31.34.0851900
体外研究：
BET-IN-12 (compound 15) (24 hours) displays BRD4 and c-Myc inhibition, MM proliferation with IC50s values of 0.9 nM, 2.0 nM, and 6.0 nM, respectively.BET-IN-12 (compound 15) (24 hours) has high oxidative stability across species and low glucuronidation across species, so that translate into low orally administered minimum efficacious doses (MEDs) .
BET-IN-12 is an orally avtive inhibitor of bromodomain and extra-terminal (BET) with an IC50 of 0.9 nM for BRD4.
体内研究：
BET-IN-12 (compound 15) is 100% oral bioavailability in mouse.BET-IN-12 (compound 15) impairs the growth of established PDX tumors (TGI = 88%) at MED = 2 mg/kg (AUC = 4800 nM?h).pharmacokinetic (PK) profile dose (iv/po, mg/kg)CLp ((mL/min)/kg)Vd (L/kg) half-life (ie, h)F (%) AUC (po, nM.h)
mouse1.0/3.04.21.43.410025000
rat1.0/5.0182.94.1746600
dog0.1/0.3135.87.673550
monkey0.1/0.34.31.34.0851900
体外研究：
BET-IN-12 (compound 15) (24 hours) displays BRD4 and c-Myc inhibition, MM proliferation with IC50s values of 0.9 nM, 2.0 nM, and 6.0 nM, respectively.BET-IN-12 (compound 15) (24 hours) has high oxidative stability across species and low glucuronidation across species, so that translate into low orally administered minimum efficacious doses (MEDs) .
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