| Field | Specification |
|---|---|
| Target | |
| Alternative names | PRN1008 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C36H40FN9O3 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Rilzabrutinib, also known as PRN1008, is a reversible covalent, selective, orally active inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 1.3 nM. It is supplied as a white to off-white solid (C36H40FN9O3, MW 665.76) at 98.97% purity.
Physical & Chemical Properties
| CAS Number | 1575596-29-0 |
|---|---|
| Molecular Formula | C36H40FN9O3 |
| Molecular Weight | 665.76 g/mol |
| Purity | 98.97% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | NC1=C2C(C3=C(C=C(OC4=CC=CC=C4)C=C3)F)=NN([C@H]5CN(CCC5)C(/C(C#N)=C/C(C)(N6CCN(C7COC7)CC6)C)=O)C2=NC=N1 |
| Target | BTK, BMX, ITK, TEC, RLK, BLK, EGFR, ERBB2, ERBB4 |
| Signaling Pathway | Protein Tyrosine Kinase/RTK |
| Solubility | In Vitro: DMSO: ≥ 130 mg/mL (195.27 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) * "≥" means soluble, but saturation unknown. |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
[1][2]
|
BTK 1.3 nM (IC50) |
BMX 1.0 nM (IC50) |
ITK 440 nM (IC50) |
TEC 0.8 nM (IC50) |
RLK 1.2 nM (IC50) |
BLK 6.3 nM (IC50) |
EGFR 520 nM (IC50) |
ERBB2 3900 nM (IC50) |
ERBB4 11.3 nM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
[2]. Hill RJ, Bradshaw JM, Bisconte A, Tam D, Owens TD, Brameld KA, Smith PF, Funk JO, Goldstein DM, Nunn PA. Preclinical Characterization of PRN1008, a Novel Reversible Covalent Inhibitor of BTK that Shows Efficacy in a RAT Model of Collagen-Induced Arthritis. Annals of the Rheumatic Diseases 2015; 74(Suppl 2): 216.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | ≥ 130 mg/mL (195.27 mM) | use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.08 mg/mL (3.12 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.08 mg/mL (3.12 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.08 mg/mL (3.12 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
Rilzabrutinib is a reversible covalent inhibitor of Bruton’s Tyrosine Kinase (BTK) with an IC50 of 1.3±0.5 nM, and it is highly selective when tested against a panel of 251 other kinases. Rilzabrutinib targets a cysteine on BTK, which gives a slow off-rate, shown by 79±2% of binding to BTK in PBMC being retained 18 hours after the compound is washed away in vitro. Covalent cysteine binding is fully reversible after the target is denatured. Rilzabrutinib inhibits anti-IgM-induced human B cell proliferation (10% serum) and B cell CD69 expression, with IC50 values of 5±2.4 nM and 123±38 nM, respectively[2].
In Vivo
In vivo, Rilzabrutinib's pharmacodynamic effects are lasting after the compound has cleared from circulation, in line with extended target residence time. Rilzabrutinib also reverses collagen-induced arthritis in rats and suppresses it completely, in a dose dependent manner, which allows target occupancy to be correlated with disease modification[2].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Bruton tyrosine kinase (Btk) in neutrophils is indispensable for initiating and maintaining skin inflammation in a model of pemphigoid diseases. Br J Pharmacol 2026 Jan 18. PMID: 41549045
Res Sq. 2026 Apr 22.
