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DS89002333 is an orally active and potent PRKACA inhibitor, with an IC 50 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) In Vitro 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). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: NIH/3T3 cells Concentration: 0.001, 0.01, 0.1, 1, 10 µM Incubation Time: 30 min Result: Showed a dose-dependent decrease in phosphorylation of CREB, with an IC 50 of 50 nM. In Vivo 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. Form:Solid IC50& Target:PRKACA 0.3 nM (IC 50 )
中文名称
DS89002333
英文名称
DS89002333
中文别名
-
英文别名
-
CAS号
2832159-79-0
分子式
C22H20ClF2N3O3
分子量
447.86 g/mol
精确质量
≥99%
PSA
-
Logp
-
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DS89002333 5mg

品牌:阿拉丁
货号:D649090-5mg
级别: ≥99%
货期:30天
已售 762 件
20161
.08
24193
.3
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5mg

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