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BLU2864 

Cat. No.: HY-150076
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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.

For research use only. We do not sell to patients.

BLU2864 Chemical Structure

BLU2864 Chemical Structure

CAS No. : 2810747-89-6

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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].

IC50 & 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

452.43

Formula

C24H19F3N4O2

CAS No.
SMILES

FC1=CC(C(F)F)=CC2=C1[[email protected]]([[email protected]@H](O)C2)NC(C(C=C3)=CN=C3C4=C(C(C)=CN5)C5=NC=C4)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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BLU2864
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HY-150076
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