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BLU2864

Catalog No. T60170 CAS 2810747-89-6

BLU2864 is an orally active, highly selective, ATP-competitive PRKACA inhibitor with IC 50 of 0.3 nM. BLU2864 exhibits anti-tumor activity. BLU2864 has potential to be used in cancer and polycystic kidney disease research [1] [2].

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BLU2864, CAS 2810747-89-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 139.00
5 mg	In stock	$ 347.00
10 mg	In stock	$ 563.00
25 mg	In stock	$ 890.00
50 mg	In stock	$ 1,230.00
100 mg	In stock	$ 1,670.00
500 mg	In stock	$ 3,350.00

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Purity: 99.73%

ee: 100%

Purity: 99.42%

Purity: 97.58%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	BLU2864 is an orally active, highly selective, ATP-competitive PRKACA inhibitor with IC 50 of 0.3 nM. BLU2864 exhibits anti-tumor activity. BLU2864 has potential to be used in cancer and polycystic kidney disease research [1] [2].
In vitro	BLU2864 (40 nM and 200 nM; 5 d) shows inhibition of forskolin -induced cystogenesis in vitro[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 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.

Molecular Weight	452.43
Formula	C24H19F3N4O2
CAS No.	2810747-89-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (110.51 mM), Sonication is recommended.

References and Literature

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. 2. Stefanie S. Schalm, et al. Evaluation of PRKACA as a Therapeutic Target for Fibrolamellar Carcinoma. bioRxiv 2022.01.31.477690.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Anti-Cancer Active Compound Library Inhibitor Library Bioactive Compounds Library Max Bioactive Compound Library Anti-Cancer Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

BLU2864 2810747-89-6 Others BLU-2864 BLU 2864 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.