产品
编 号：F763038
分子式：C22H20ClF2N3O3
分子量：447.86
分子式：C22H20ClF2N3O3
分子量：447.86
产品类型
规格
价格
是否有货
1mg
询价
询价
结构图
CAS No: 2832159-79-0
产品详情
生物活性：
DS89002333 is an orally active and potent PRKACA inhibitor, with an IC50 of 0.3 nM. DS89002333 shows good anti-tumor activity in an FL-HCC patient-derived xenograft model (expressing the DNAJB1-PRKACA fusion gene). DS89002333 can be used in study of fibrolamellar hepatocellular carcinoma (FL-HCC).
体内研究：
DS89002333 (12.5, 50 mg/kg; p.o.; twice daliy for 5 days) shows anti-tumor activity in an NIH/3T3-fusion allograft model.DS89002333 (3, 30 mg/kg; p.o.; twice daliy for 22 days) shows significant anti-tumor activity in FL-HCC PDX xenograft model.Animal Model:Female nude mice (NIH/3T3-fusion allograft model).
Dosage:12.5, 50 mg/kg
Administration:Oral administration, twice daliy for 5 days.
Result:Exhibited anti-tumor activity without body weight loss.
Animal Model:Female NOD SCID mice (FL-HCC PDX xenograft model).
Dosage:3, 30 mg/kg
Administration:Oral administration, twice daliy for 22 days.
Result:Significant inhibited tumor in mice, and showed temporary body weight loss (at 30 mg/kg), but this resolved following continuous dosing.
体外研究：
DS89002333 (0.001, 0.01, 0.1, 1, 10 μM; 30 min) inhibits phosphorylation of CREB in a dose-dependent manner in NIH/3T3 cells (phosphorylation status of CREB as a marker of intracellular PRAKACA inhibitory activity).
DS89002333 is an orally active and potent PRKACA inhibitor, with an IC50 of 0.3 nM. DS89002333 shows good anti-tumor activity in an FL-HCC patient-derived xenograft model (expressing the DNAJB1-PRKACA fusion gene). DS89002333 can be used in study of fibrolamellar hepatocellular carcinoma (FL-HCC).
体内研究：
DS89002333 (12.5, 50 mg/kg; p.o.; twice daliy for 5 days) shows anti-tumor activity in an NIH/3T3-fusion allograft model.DS89002333 (3, 30 mg/kg; p.o.; twice daliy for 22 days) shows significant anti-tumor activity in FL-HCC PDX xenograft model.Animal Model:Female nude mice (NIH/3T3-fusion allograft model).
Dosage:12.5, 50 mg/kg
Administration:Oral administration, twice daliy for 5 days.
Result:Exhibited anti-tumor activity without body weight loss.
Animal Model:Female NOD SCID mice (FL-HCC PDX xenograft model).
Dosage:3, 30 mg/kg
Administration:Oral administration, twice daliy for 22 days.
Result:Significant inhibited tumor in mice, and showed temporary body weight loss (at 30 mg/kg), but this resolved following continuous dosing.
体外研究：
DS89002333 (0.001, 0.01, 0.1, 1, 10 μM; 30 min) inhibits phosphorylation of CREB in a dose-dependent manner in NIH/3T3 cells (phosphorylation status of CREB as a marker of intracellular PRAKACA inhibitory activity).
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