BLU2864 是一种具有口服活性的、高选择性的、ATP 竞争性的 PRKACA 抑制剂 (IC50=0.3 nM)。BLU2864 具有抗肿瘤活性，可用于癌症和多囊肾的研究。

BLU2864 is an orally active, highly selective, ATP-competitive inhibitor of PRKACA with IC50 of 0.3 nM. BLU2864 exhibits anti-tumor activity. BLU2864 has research value in cancer and polycystic kidney disease research.

BLU2864 inhibits forskolin induced cystogenesis of mIMCD3 cells by 72% and 100% at 40 and 200 nM, respectively[1].

Compared with control mice, BLU2864 treatment (Oral gavage; 45 mg/kg; once daily; 5 days) inhibits kidney basal and total PKA activities by 74% and 87% at 3 hours and by 46% and 56% at 15 hours, respectively. Compared with control mice, BLU2864-treated mice (Oral gavage; 30 mg/kg; once daily; 5 days) showed higher urine outputs, lower kidney weights, kidney volumes as percent of body weights, and cyst indices. Renal basal and total PKA activities by 69% and 84% is lower in the BLU2864-treated mice compared with controls[1]. BLU2864 (Oral gavage; 30 mg/kg and 75 mg/kg; once daily; 34 days) inhibited tumor growth by 48.5% (P=0.003) and by 45.3% (P=0.0005), respectively[2].

2810747-89-6

C24H19F3N4O2

452.43

BLU2864

DMSO:40mg/mL,Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years