DS89002333

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 )

No numbering system information yet

No physical and chemical property information yet

No safety information yet

No production method and use information yet

No upstream information yet

No downstream information yet

No related product information yet