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Rilzabrutinib

Name: Rilzabrutinib
Brand: TargetMol
SKU: T12542
Price: 100 USD
Availability: InStock
Rating: 5 (10 reviews)

(Synonyms: PRN1008) Copy Product Info

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Synonyms: PRN1008

Catalog No. T12542 Copy Product Info

Purity: 99.76%

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Rilzabrutinib (PRN1008) is a small-molecule inhibitor and a reversible covalent inhibitor of Bruton's tyrosine kinase (BTK) (IC50 = 1.3 nM), featuring high selectivity, oral activity, and favorable cell permeability, exhibiting anti-inflammatory and immunomodulatory activities.

Cas No. 1575596-29-0

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Pack Size	Price	USA Stock	Global Stock
1 mg	$100	In Stock	In Stock
5 mg	$247	In Stock	In Stock
10 mg	$396	In Stock	In Stock
25 mg	$689	In Stock	In Stock
50 mg	$993	In Stock	In Stock
100 mg	$1,390	-	In Stock
500 mg	$2,780	-	In Stock
1 mL x 10 mM (in DMSO)	$362	In Stock	In Stock

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

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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

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

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Purity:99.76%

Color:White

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COA HNMR HPLC

Product Introduction

Rilzabrutinib AI Summary

Rilzabrutinib exhibits potent inhibitory activity against Bruton's Tyrosine Kinase (BTK) with an IC50 ranging from 1.3 to 1.5 nM, as determined by various assays including Caliper-Based Kinase Assays. It demonstrates a high binding affinity with a fast on-rate constant of 5.1 x 10^4/M/s and a slow off-rate constant of 1.2 x 10^4/M/s. In vivo studies, particularly in a rat model of collagen-induced arthritis, confirm its efficacy, showing dose-dependent BTK inhibition. The compound also possesses suitable oral bioavailability, favorable permeability characteristics, and solubility, indicating strong potential for further development as a BTK inhibitor..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Rilzabrutinib (PRN1008) is a small-molecule inhibitor and a reversible covalent inhibitor of Bruton's tyrosine kinase (BTK) (IC50 = 1.3 nM), featuring high selectivity, oral activity, and favorable cell permeability, exhibiting anti-inflammatory and immunomodulatory activities.
Targets & IC50	BTK (Ramos B cell):8 ± 2 nM, RLK:1.2 nM, BMX?kinase:1.0 ± 0.1 nM, BLK:6.3 nM, FcγR (Monocyte):56 ± 45 nM, BCR (B cell):5 ± 2 nM, ERBB2:3900 nM, TEC:0.8 nM, ERBB4:11.3 nM, EGFR:520 nM, BTK:1.3 nM, ITK:440 nM, TXK:1.2 ± 0.3 nM
In vitro	Methods:The inhibitory effects of Rilzabrutinib were evaluated in human whole blood B cell activation assays (anti-IgM stimulation for 18 h), isolated B cell proliferation assays (anti-IgM stimulation for 48 h), monocyte FcγR activation assays (IgG stimulation for 4 h), and basophil FcεR activation assays (anti-IgE stimulation for 15 min). Results: The IC₅₀ values of Rilzabrutinib in the above assays were 123 nM, 5 nM, 56 nM, and 490 nM, respectively, all showing concentration-dependent inhibitory effects. [1]
In vivo	Methods: In a collagen-induced arthritis rat model, Rilzabrutinib was administered orally at 10–40 mg/kg once or twice daily (vehicle: citric acid water); in an ITP mouse model, Rilzabrutinib was administered orally at 10–40 mg/kg once daily; in a canine pemphigus model, Rilzabrutinib was administered orally at 15–30 mg/kg/day. Results: Rilzabrutinib dose-dependently improved arthritis scores and pathology in rats, reduced platelet loss in mice, and significantly improved clinical symptoms in dogs within 2 weeks. [1]
Synonyms	PRN1008

Chemical Properties

Molecular Weight	665.76
Formula	C₃₆H₄₀FN₉O₃
Cas No.	1575596-29-0
Smiles	CC(C)(\C=C(/C#N)C(=O)N1CCC[C@H](C1)n1nc(-c2ccc(Oc3ccccc3)cc2F)c2c(N)ncnc12)N1CCN(CC1)C1COC1
Relative Density.	1.39 g/cm3 (Predicted)

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 240 mg/mL (360.49 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (7.51 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	1.5020 mL	7.5102 mL	15.0204 mL	75.1021 mL
5 mM	0.3004 mL	1.5020 mL	3.0041 mL	15.0204 mL
10 mM	0.1502 mL	0.7510 mL	1.5020 mL	7.5102 mL
20 mM	0.0751 mL	0.3755 mL	0.7510 mL	3.7551 mL
50 mM	0.0300 mL	0.1502 mL	0.3004 mL	1.5020 mL
100 mM	0.0150 mL	0.0751 mL	0.1502 mL	0.7510 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.

Dose Conversion

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

Keywords

TECRLKRilzabrutinibPRN-1008PRN 1008ITKInhibitorinhibitHER4ERBB4ERbB2EGFRBTKBruton tyrosine kinaseBMXBLK

Related Tags: Rilzabrutinib chemical structure | Rilzabrutinib in vivo | Rilzabrutinib in vitro | Rilzabrutinib formula | Rilzabrutinib molecular weight