2810747-89-6
2810747-89-6 structure
- Name: BLU2864
- Chemical Name: BLU2864
- CAS Number: 2810747-89-6
- Molecular Formula: C24H19F3N4O2
- Molecular Weight: 452.43
- Catalog: Research Areas Cancer
- Create Date: 2022-10-12 11:25:06
- Modify Date: 2025-08-26 09:19:17
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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[1][2].
| Name | BLU2864 |
|---|
| Description | 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[1][2]. |
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| Related Catalog | |
| Target |
IC50: 0.3 nM (PRKACA)[2] |
| In Vitro | BLU2864 (40 nM and 200 nM; 5 d) inhibits forskolin (HY-15371)-induced in vitro cystogenesis[1]. Cell Viability Assay[1] 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. |
| In Vivo | BLU2864 (oral gavage; 45 mg/kg; once daily; 5 d) inhibits renal PKA activity in Pkd1RC/RC mice[1]. BLU2864 (oral gavage; 30 mg/kg; once daily; 5 d) inhibits PKA activity and ameliorates PKD in Pkd1RC/RC mice[1]. BLU2864 (oral gavage; 30 mg/kg and 75 mg/kg; once daily; 34 d) reduces FLC tumor growth in vivo[2]. Animal Model: Pkd1RC/RC mice[1] 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[1] 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[2] 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. |
| References |
| Molecular Formula | C24H19F3N4O2 |
|---|---|
| Molecular Weight | 452.43 |