BLU2864

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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 PRKACA inhibitor (IC50=0.3 nM). BLU2864 shows anti-tumor activity. BLU2864 can be used in cancer and polycystic kidney disease research.

BLU2864 (40 nM and 200 nM; 5 d) inhibits forskolin (HY-15371)-induced in vitro cystogenesis.Cell Viability Assay Cell Line:mIMCD3 cells Concentration:40 nM and 200 nM Incubation Time:5 days Result:Inhibited forskolin induced in vitro cystogenesis of mIMCD3 cells cultured in Matrigel by 72% and 100% at 40 and 200 nM concentrations, respectively, relative to control.

BLU2864 (oral gavage; 45 mg/kg; once daily; 5 d) inhibits renal PKA activity in Pkd1RC/RC mice.BLU2864 (oral gavage; 30 mg/kg; once daily; 5 d) inhibits PKA activity and ameliorates PKD in Pkd1RC/RC mice. BLU2864 (oral gavage; 30 mg/kg and 75 mg/kg; once daily; 34 d) reduces FLC tumor growth in vivo.Animal Model:Pkd1RC/RC mice Dosage:45 mg/kg Administration:Oral gavage; 45 mg/kg; once daily; 5 days Result: Suppressed kidney basal and total PKA activities by 74% and 87% at 3 hours and by 46% and 56% at 15 hours, respectively, in the BLU2864-treated mice compared with controls.Animal Model:Pkd1RC/RC mice Dosage:30 mg/kg Administration:Oral gavage; 30 mg/kg; once daily; 5 days Result:Showed higher urine outputs at 15 weeks in the BLU2864-treated mice than in the controls. Showed lower kidney weights, kidney volumes as percent of body weights, and cyst indices. Showed renal basal and total PKA activities by 69% and 84% lower in the BLU2864-treated mice compared with controls.Animal Model:Mice harboring FLC PDX tumors Dosage:30 mg/kg and 75 mg/kg Administration:Oral gavage; 30 mg/kg and 75 mg/kg; once daily; 34 days Result:Inhibited tumor growth by 48.5% (P=0.003) and by 45.3% (P=0.0005), respectively, at day 34.

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2810747-89-6

452.43

C24H19F3N4O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (221.03 mM; 超声助溶 )

N(C(=O)C=1C=CC(=NC1)C2=C3C(NC=C3C)=NC=C2)[C@@H]4C=5C(=CC(C(F)F)=CC5F)C[C@@H]4O

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(-20℃)

With Ice Pack

≥ 2 years