
BLU2864
CAS No. 2810747-89-6
BLU2864( —— )
Catalog No. M35362 CAS No. 2810747-89-6
BLU2864 is an orally active, highly selective, ATP-competitive PRKACA inhibitor with an IC50 of 0.3 nM, exhibiting anti-tumor activity and potential applications in cancer and polycystic kidney disease research .
Purity : >98% (HPLC)






Size | Price / USD | Stock | Quantity |
2MG | 126 | Get Quote |
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5MG | 198 | Get Quote |
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10MG | 321 | Get Quote |
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25MG | 490 | Get Quote |
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50MG | 679 | Get Quote |
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100MG | 900 | Get Quote |
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200MG | 1215 | Get Quote |
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500MG | Get Quote | Get Quote |
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1G | Get Quote | Get Quote |
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Biological Information
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Product NameBLU2864
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NoteResearch use only, not for human use.
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Brief DescriptionBLU2864 is an orally active, highly selective, ATP-competitive PRKACA inhibitor with an IC50 of 0.3 nM, exhibiting anti-tumor activity and potential applications in cancer and polycystic kidney disease research .
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DescriptionBLU2864 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.
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In VitroBLU2864 (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.
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In VivoBLU2864 (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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Synonyms——
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PathwayOthers
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TargetOther Targets
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RecptorOthers
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Research Area——
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Indication——
Chemical Information
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CAS Number2810747-89-6
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Formula Weight452.43
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Molecular FormulaC24H19F3N4O2
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 100 mg/mL (221.03 mM; Ultrasonic )
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SMILESN(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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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Xiaofang Wang, et al. Protein Kinase A Downregulation Delays the Development and Progression of Polycystic Kidney Disease. J Am Soc Nephrol. 2022 Jun;33(6):1087-1104.?
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