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BLU0588

Catalog No. T60169 CAS 2810747-78-3

BLU0588 is a selective PRKACA inhibitor. BLU0588 inhibits PRKACA catalytic activity with a half-maximal inhibitory concentration (IC50) of 1 nM.

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BLU0588, CAS 2810747-78-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 195.00
5 mg	In stock	$ 448.00
10 mg	In stock	$ 658.00
25 mg	In stock	$ 987.00
50 mg	In stock	$ 1,380.00
100 mg	In stock	$ 1,890.00
500 mg	In stock	$ 3,780.00
1 mL * 10 mM (in DMSO)	In stock	$ 497.00

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Purity: 98.25%

ee: 100%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	BLU0588 is a selective PRKACA inhibitor. BLU0588 inhibits PRKACA catalytic activity with a half-maximal inhibitory concentration (IC50) of 1 nM.
In vitro	RKACA cellular IC50 values were 25.0 nM with BLU0588, which were determined from inhibition of VASP Ser157 phosphorylation in forskolin-stimulated Huh7 cells[1].
In vivo	For in vivo studies, mice were given either BLU0588 at 30 mg/kg and 75 mg/kg once daily (QD) and monitored for 24 hours. Plasma concentrations peaked within 2–4 hours of QD dosing. For BLU0588-treated mice, phosphorylated VASP was reduced to 19% and 4% of baseline phosphorylation levels with 30 mg/kg QD and 75 mg/kg QD, respectively, 4 hours after dosing; phosphorylated VASP levels fully recovered by 24 hours post administration of 30 mg/kg QD. When mice harboring FLC PDX tumors were treated with BLU0588 given orally at 30 mg/kg QD, by Day 34 tumor growth was inhibited by 48.5% (P = 0.003)[1].

Molecular Weight	423.51
Formula	C26H25N5O
CAS No.	2810747-78-3

Storage

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

Solubility Information

DMSO: 55 mg/mL (129.87 mM)

References and Literature

1. 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 Inhibitor Library Bioactive Compounds Library Max Bioactive 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

BLU0588 2810747-78-3 Others BLU 0588 BLU-0588 inhibitor inhibit

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