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BLU0588

Name: BLU0588
Brand: TargetMol
SKU: T60169
Price: 1890 USD
Availability: InStock
Rating: 5 (10 reviews)

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Synonyms:

Catalog No. T60169 Copy Product Info

Purity: 99.85%

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BLU0588 is a small-molecule inhibitor and a PRKACA-targeted inhibitor (IC50 = 1 nM, Kd = 4 nM), featuring high selectivity, cell permeability, and oral activity, suitable for experimental research and therapeutic development in fibrolamellar hepatocellular carcinoma (FLC).

Cas No. 2810747-78-3

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Pack Size	Price	USA Stock	Global Stock
1 mg	$195	In Stock	In Stock
5 mg	$448	In Stock	In Stock
10 mg	$658	In Stock	In Stock
25 mg	$987	-	In Stock
50 mg	$1,380	-	In Stock
100 mg	$1,890	-	In Stock
500 mg	Inquiry	Inquiry	Inquiry
1 mL x 10 mM (in DMSO)	$497	In Stock	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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Custom-made molecule. TargetMol’s expert synthesis team delivers cost-effective solutions. Contact us for inquiries. Committed to serving you.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Batch Information

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Purity:99.85%

ee:100%

Appearance:Solid

Color:Yellow

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COA HNMR LCMS CSFC

Product Introduction

Bioactivity

Description	BLU0588 is a small-molecule inhibitor and a PRKACA-targeted inhibitor (IC50 = 1 nM, Kd = 4 nM), featuring high selectivity, cell permeability, and oral activity, suitable for experimental research and therapeutic development in fibrolamellar hepatocellular carcinoma (FLC).
Targets & IC50	PRKACA:1 nM, PRKACA:4 nM (Kd), RKACA (PHOS cellsphorylation of VASP Ser157 in Huh7 cells):25.0 nM
In vitro	Methods: In FLC PDX cells, BLU0588 (1.5 μM) was used to treat for 1 day or 14 days, and gene expression analysis was performed to detect its effect on FLC-specific gene signatures; additionally, different concentrations of BLU0588 (0–312.5 nM) were used to detect changes in pVASP levels. Results: BLU0588 reversed FLC-specific gene signatures, downregulating genes overexpressed in FLC (such as CPS1 and G6PC) and upregulating genes underexpressed in FLC; pVASP levels were reduced in a dose-dependent manner.[1]
In vivo	Methods: The inhibitory effect of single oral administration of BLU0588 (30–75 mg/kg) on PRKACA signaling was assessed; the maximum tolerated dose in mice was determined through continuous administration for over 3 weeks; and antitumor efficacy was evaluated in tumor models with oral BLU0588 (30 mg/kg, once daily for 34 days). Results: BLU0588 effectively inhibited downstream PRKACA signaling, with phosphorylated VASP levels returning to baseline within 24 hours; the maximum tolerated dose for continuous administration was 30 mg/kg QD; and tumor growth in mice was significantly suppressed. [1]

Chemical Properties

Molecular Weight	423.51
Formula	C₂₆H₂₅N₅O
Cas No.	2810747-78-3
Smiles	O=C(N[C@@H]1C2=C(C=CC=C2)C[C@H]1N1CCCC1)C1=CC=C(C2=C3C=CNC3=NC=C2)N=C1
Relative Density.	1.35 g/cm3 at 20℃ (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 85.8 mg/mL (202.59 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3612 mL	11.8061 mL	23.6122 mL	118.0610 mL
5 mM	0.4722 mL	2.3612 mL	4.7224 mL	23.6122 mL
10 mM	0.2361 mL	1.1806 mL	2.3612 mL	11.8061 mL
20 mM	0.1181 mL	0.5903 mL	1.1806 mL	5.9030 mL
50 mM	0.0472 mL	0.2361 mL	0.4722 mL	2.3612 mL
100 mM	0.0236 mL	0.1181 mL	0.2361 mL	1.1806 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.