产品
编 号：F751781
分子式：C27H23F4N5O4
分子量：557.5
分子式：C27H23F4N5O4
分子量：557.5
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CAS No: 2379416-48-3
产品详情
生物活性：
B026 is a selective, potent, orally active p300/CBP histone acetyltransferase (HAT) inhibitor with IC50 values of 1.8 nM and 9.5 nM for p300 and CBP enzyme, respectively. B026 has anticancer activity for androgen receptor-positive (AR+) prostate cancer cell lines.
体内研究：
B026 (1-3 mg/kg; i.v. and p.o.; 0-24 h; male SD rats) has a low clearance (13.4 mL/min/kg) and good oral exposure (AUC=3.71 μM·h) with good oral bioavailability (F=56%) in rat.B026 (50-100 mg/kg; p.o.; daily, for 28 days; balb/c female mice) inhibits tumor growth in a dose-dependent manner.Animal Model:Balb/c female mice with MV-4-11 xenograft
Dosage:50 and 100 mg/kg
Administration:Oral administration; daily, for 28 days
Result:Inhibited tumor growth with TGI of 75.0% at 50 mg/kg and 85.7% at 100 mg/kg, respectively.
Animal Model:Male SD rats
Dosage:1 and 3 mg/kg
Administration:Intravenous injection and oral administration; 0.25, 0.5 , 1 , 2 , 4 , 8 and 24 hours
Result:1.19 Administrationi.v. (1 mg/kg)p.o. (3 mg/kg)
T1/2 (h)1.51.02
Tmax (h)0.83
Cmax (μM)1.12
AUClast (μM·h)2.223.71
Vdss (L/kg)1.5
CL_obs (mL/min/kg)13.4
PPB %98.2F %56
体外研究：
B026 (0-5 μM; 12 h; cancer cell lines) has antiproliferative activity.B026 (0-5 μM; 6 h; MV-4-11 cells) exhibits inhibitory effects on H3K27Ac expression.B026 (0-5 μM; 12 h; MV-4-11 cells) targets the cellular p300 protein and increases the thermal stability of p300 protein in a dose-dependent manner.B026 (0-1 μM; 24 h; MV-4-11 cells) decreases the expression of MYC, which a key oncogenictranscription factor that is regulated by superenhancer regions containing p300/CBP.
B026 is a selective, potent, orally active p300/CBP histone acetyltransferase (HAT) inhibitor with IC50 values of 1.8 nM and 9.5 nM for p300 and CBP enzyme, respectively. B026 has anticancer activity for androgen receptor-positive (AR+) prostate cancer cell lines.
体内研究：
B026 (1-3 mg/kg; i.v. and p.o.; 0-24 h; male SD rats) has a low clearance (13.4 mL/min/kg) and good oral exposure (AUC=3.71 μM·h) with good oral bioavailability (F=56%) in rat.B026 (50-100 mg/kg; p.o.; daily, for 28 days; balb/c female mice) inhibits tumor growth in a dose-dependent manner.Animal Model:Balb/c female mice with MV-4-11 xenograft
Dosage:50 and 100 mg/kg
Administration:Oral administration; daily, for 28 days
Result:Inhibited tumor growth with TGI of 75.0% at 50 mg/kg and 85.7% at 100 mg/kg, respectively.
Animal Model:Male SD rats
Dosage:1 and 3 mg/kg
Administration:Intravenous injection and oral administration; 0.25, 0.5 , 1 , 2 , 4 , 8 and 24 hours
Result:1.19 Administrationi.v. (1 mg/kg)p.o. (3 mg/kg)
T1/2 (h)1.51.02
Tmax (h)0.83
Cmax (μM)1.12
AUClast (μM·h)2.223.71
Vdss (L/kg)1.5
CL_obs (mL/min/kg)13.4
PPB %98.2F %56
体外研究：
B026 (0-5 μM; 12 h; cancer cell lines) has antiproliferative activity.B026 (0-5 μM; 6 h; MV-4-11 cells) exhibits inhibitory effects on H3K27Ac expression.B026 (0-5 μM; 12 h; MV-4-11 cells) targets the cellular p300 protein and increases the thermal stability of p300 protein in a dose-dependent manner.B026 (0-1 μM; 24 h; MV-4-11 cells) decreases the expression of MYC, which a key oncogenictranscription factor that is regulated by superenhancer regions containing p300/CBP.
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