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BLU2864

Name: BLU2864
Brand: TargetMol
SKU: T60170
Price: 83 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T60170Cas 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 [1] [2].

BLU2864

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Purity: 99.92%

Catalog No. T60170Cas No. 2810747-89-6

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$83	In Stock	In Stock
5 mg	$208	In Stock	In Stock
10 mg	$338	In Stock	In Stock
25 mg	$533	In Stock	In Stock
50 mg	$738	In Stock	In Stock
100 mg	$1,000	In Stock	In Stock
200 mg	$1,350	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.92%

Appearance:Solid

Color:White to Yellow

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	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 [1] [2].
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[1].
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.

Chemical Properties

Molecular Weight	452.43
Formula	C₂₄H₁₉F₃N₄O₂
Cas No.	2810747-89-6
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
Relative Density.	1.48 g/cm3 (Predicted)

Storage & Solubility Information

Storage

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

Solubility Information

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

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.42 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2103 mL	11.0514 mL	22.1029 mL	110.5143 mL
5 mM	0.4421 mL	2.2103 mL	4.4206 mL	22.1029 mL
10 mM	0.2210 mL	1.1051 mL	2.2103 mL	11.0514 mL
20 mM	0.1105 mL	0.5526 mL	1.1051 mL	5.5257 mL
50 mM	0.0442 mL	0.2210 mL	0.4421 mL	2.2103 mL
100 mM	0.0221 mL	0.1105 mL	0.2210 mL	1.1051 mL

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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.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

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