产品
编 号：F755491
分子式：C29H26N6O3
分子量：506.56
分子式：C29H26N6O3
分子量：506.56
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CAS No: 2758117-74-5
产品详情
生物活性：
PARP1/BRD4-IN-1 is a potent and high selective PARP1/BRD4 inhibitor (IC50s of 49 and 202 nM in PARP1 and BRD4, respectively). PARP1/BRD4-IN-1 represses the expression and activity of PARP1 and BRD4 to synergistically inhibit the malignant growth of pancreatic cancer cells.
体内研究：
PARP1/BRD4-IN-1 (30mg/kg; intraperitoneal injection for 28 days) can significantly inhibit the tumor size and weight, and does not cause significant damage of the kidney, lung, spleen, liver and heart in mice.Animal Model:Athymic nude mice (6-7 weeks, 18-20 g, SW1990-injected)
Dosage:30mg/kg
Administration:Intraperitoneal injection for 28 days
Result:Significantly inhibited the tumor size and weight and did not cause significant damage of the kidney, lung, spleen, liver and heart.
体外研究：
PARP1/BRD4-IN-1 (compound III-7) (0-2 μM; 3-7 days) has potent inhibition of the growth of cancer cell lines.PARP1/BRD4-IN-1 (0, 1, 2 μM; 4 days) can significantly inhibit the expression of PARP1 and BRD4 at 2 μM in SW1990 cells.PARP1/BRD4-IN-1 (1, 2 μM; 4 days) arrests the cell cycle at G0/G1 and G2/M phase in SW1990 cells.PARP1/BRD4-IN-1 (0, 1, 2 μM; 4 days) has the potent efficacy on the apoptosis of SW1990 cells at 2 μM.PARP1/BRD4-IN-1 (1, 2 μM; 4 days) regulates the expression of HEXIM1, c-Myc, FOXO1, MDC1 and TOPBP1 to enhance the inhibition of DNA repair in SW1990 cells.
PARP1/BRD4-IN-1 is a potent and high selective PARP1/BRD4 inhibitor (IC50s of 49 and 202 nM in PARP1 and BRD4, respectively). PARP1/BRD4-IN-1 represses the expression and activity of PARP1 and BRD4 to synergistically inhibit the malignant growth of pancreatic cancer cells.
体内研究：
PARP1/BRD4-IN-1 (30mg/kg; intraperitoneal injection for 28 days) can significantly inhibit the tumor size and weight, and does not cause significant damage of the kidney, lung, spleen, liver and heart in mice.Animal Model:Athymic nude mice (6-7 weeks, 18-20 g, SW1990-injected)
Dosage:30mg/kg
Administration:Intraperitoneal injection for 28 days
Result:Significantly inhibited the tumor size and weight and did not cause significant damage of the kidney, lung, spleen, liver and heart.
体外研究：
PARP1/BRD4-IN-1 (compound III-7) (0-2 μM; 3-7 days) has potent inhibition of the growth of cancer cell lines.PARP1/BRD4-IN-1 (0, 1, 2 μM; 4 days) can significantly inhibit the expression of PARP1 and BRD4 at 2 μM in SW1990 cells.PARP1/BRD4-IN-1 (1, 2 μM; 4 days) arrests the cell cycle at G0/G1 and G2/M phase in SW1990 cells.PARP1/BRD4-IN-1 (0, 1, 2 μM; 4 days) has the potent efficacy on the apoptosis of SW1990 cells at 2 μM.PARP1/BRD4-IN-1 (1, 2 μM; 4 days) regulates the expression of HEXIM1, c-Myc, FOXO1, MDC1 and TOPBP1 to enhance the inhibition of DNA repair in SW1990 cells.
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