BLU2864

SKU: orb1819252

Description

BLU2864 is a potent and selective ATP-competitive inhibitor of PRKACA (IC₅₀ = 0.3 nM). It demonstrates anti-tumor activity in preclinical research, supporting its investigation for applications in oncology and polycystic kidney disease models, both in vitro and in vivo.

Research Area

Signal Transduction

Key Properties

• CAS Number: 2810747-89-6
• MW: 452.43
• Purity: 97.58% (May vary between batches)
• Formula: C₂₄H₁₉F₃N₄O₂
• SMILES: 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
• Target: Others,PKA
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.42 mM);DMSO:50 mg/mL (110.51 mM)

Bioactivity

• In Vivo:
  BLU2864 administered via oral gavage at doses of 45 mg/kg and 30 mg/kg once daily for 5 days showed significant inhibition of renal PKA activity and amelioration of polycystic kidney disease (PKD) in Pkd1 RC/RC mice, indicated by reduced kidney basal and total PKA activities, decreased kidney weights, volumes relative to body weights, and cyst indices. Kidney basal and total PKA activities were suppressed significantly in treated mice compared to controls, with a noted increase in urine output and improved PKD symptoms at a dosage of 30 mg/kg. Additionally, BLU2864 treatment at dosages of 30 mg/kg and 75 mg/kg once daily for 34 days effectively retarded FLC tumor growth in vivo in mice bearing FLC PDX tumors, achieving tumor growth inhibition rates of 48.5% and 45.3%, respectively.
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• In Vitro:
  BLU2864 (40 nM and 200 nM; 5 d) inhibits forskolin-induced cystogenesis in vitro, reducing cyst formation in mIMCD3 cells cultured in Matrigel by 72% and 100% at 40 nM and 200 nM, respectively, compared to control.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BLU 2864, BLU2864, BLU-2864, PRKACA

Compound Identifiers

PubChem CID

164603354