Home Cart Sign in  
Chemical Structure| 1971920-73-6 Chemical Structure| 1971920-73-6

Structure of Tolebrutinib
CAS No.: 1971920-73-6

Chemical Structure| 1971920-73-6

*Storage: {[sel_prStorage]}

*Shipping: {[sel_prShipping]}

,{[proInfo.pro_purity]}

Tolebrutinib is a Bruton tyrosine kinase (BTK) inhibitor that can penetrate the blood-brain barrier, significant for multiple sclerosis research.

Synonyms: SAR442168; PRN2246

4.5 *For Research Use Only !

{[proInfo.pro_purity]}
Cat. No.: {[proInfo.prAm]} Purity: {[proInfo.pro_purity]}

Change View

Size Price VIP Price

US Stock

Global Stock

In Stock
{[ item.pr_size ]} Inquiry {[ getRatePrice(item.pr_usd,item.pr_rate,item.mem_rate,item.pr_is_large_size_no_price, item.vip_usd) ]}

US Stock: ship in 0-1 business day
Global Stock: ship in 5-7 days

  • {[ item.pr_size ]}

In Stock

- +

Please Login or Create an Account to: See VIP prices and availability

US Stock: ship in 0-1 business day
Global Stock: ship in 2 weeks

  • 1-2 Day Shipping
  • High Quality
  • Technical Support
Product Citations

Alternative Products

Product Details of Tolebrutinib

CAS No. :1971920-73-6
Formula : C26H25N5O3
M.W : 455.51
SMILES Code : NC1=C2C(N(C(=O)N2C3=CC=C(OC4=CC=CC=C4)C=C3)[C@]5(CN(C(C=C)=O)CCC5)[H])=CC=N1
Synonyms :
SAR442168; PRN2246
MDL No. :MFCD32710277
InChI Key :KOEUOFPEZFUWRF-LJQANCHMSA-N
Pubchem ID :124111565

Safety of Tolebrutinib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of Tolebrutinib

RTK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Primary mouse microglia 100 nM 15 minutes To evaluate the effect of tolebrutinib on BTK phosphorylation after IgG stimulation, results showed that tolebrutinib blocked the increase in BTK phosphorylation. Nat Commun. 2024 Nov 22;15(1):10116
BV-2 mouse microglial cell line 0.005-200 nM 30 minutes To evaluate the effect of PRN2675 on BTK autophosphorylation, results showed that PRN2675 rapidly reduced levels of phosphorylated BTK (Tyr223). Nat Commun. 2024 Nov 22;15(1):10116
Human induced pluripotent stem cell (hiPSC)-derived microglia 100 nM 6 hours To evaluate the effect of tolebrutinib on the transcriptional response after FcγR stimulation, results showed that tolebrutinib significantly altered the microglial transcriptome. Nat Commun. 2024 Nov 22;15(1):10116

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Experimental autoimmune encephalomyelitis (EAE) model Oral 15 mg/kg Once daily for 10 days To evaluate the effect of PRN2675 on disease manifestations in the EAE model, results showed that PRN2675 significantly reduced clinical disease scores and plasma neurofilament heavy chain (NfH) levels. Nat Commun. 2024 Nov 22;15(1):10116

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT04171310 Multiple Sclerosis PHASE1 COMPLETED 2019-12-30 Investigational Site Number 82... More >>60001, Nottingham, United Kingdom Less <<
NCT03996291 Relapsing Multiple Sclerosis PHASE2 COMPLETED 2024-11-26 North Central Neurology Associ... More >>ates, PC Site Number : 8400005, Cullman, Alabama, 35058, United States|Neurology Associates, PA Site Number : 8400002, Maitland, Florida, 32761, United States|University of South Florida Site Number : 8400009, Tampa, Florida, 33612, United States|Velocity Clinical Research Site Number : 8400007, Savannah, Georgia, 31406, United States|Consultants In Neurology Site Number : 8400001, Northbrook, Illinois, 60062, United States|UC Health, LLC Site Number : 8400008, Dayton, Ohio, 45417, United States|MDH Research LLC Site Number : 8400006, Westerville, Ohio, 43081, United States|Neurology PC Site Number : 8400003, Knoxville, Tennessee, 37922, United States|Investigational Site Number : 1240003, Vancouver, British Columbia, V6T 2B5, Canada|Investigational Site Number : 1240001, Greenfield Park, Quebec, J4V 2J2, Canada|Investigational Site Number : 2030007, Brno, 62500, Czechia|Investigational Site Number : 2030004, Hradec Kralove, 50005, Czechia|Investigational Site Number : 2030003, Jihlava, 58633, Czechia|Investigational Site Number : 2030005, Ostrava - Poruba, 70852, Czechia|Investigational Site Number : 2030006, Pardubice, 53203, Czechia|Investigational Site Number : 2030001, Praha 2, 12808, Czechia|Investigational Site Number : 2030002, Praha 5 - Motol, 15006, Czechia|Investigational Site Number : 2330001, Tallinn, 11315, Estonia|Investigational Site Number : 2500004, Nancy, 54035, France|Investigational Site Number : 5280001, Amsterdam, 1081 HV, Netherlands|Investigational Site Number : 6430006, Kazan, 420032, Russian Federation|Investigational Site Number : 6430003, Moscow, 125367, Russian Federation|Investigational Site Number : 6430001, Saint-Petersburg, 197110, Russian Federation|Investigational Site Number : 6430005, St-Petersburg, 194044, Russian Federation|Investigational Site Number : 6430007, Tyumen, 625000, Russian Federation|Investigational Site Number : 7240003, Sevilla, Andalucia, 41009, Spain|Investigational Site Number : 7240002, Barcelona, Barcelona [Barcelona], 08035, Spain|Investigational Site Number : 7240005, Salt, Girona [Gerona], 17190, Spain|Investigational Site Number : 7240001, Madrid, 28007, Spain|Investigational Site Number : 7240004, Murcia, 30120, Spain|Investigational Site Number : 8040002, Chernivtsi, 58000, Ukraine|Investigational Site Number : 8040005, Dnipro, 49038, Ukraine|Investigational Site Number : 8040001, Lviv, 79010, Ukraine|Investigational Site Number : 8040006, Lviv, 79013, Ukraine|Investigational Site Number : 8040009, Odesa, 65025, Ukraine|Investigational Site Number : 8040003, Vinnytsya, 21005, Ukraine|Investigational Site Number : 8040007, Zhytomyr, 10002, Ukraine Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.20mL

0.44mL

0.22mL

10.98mL

2.20mL

1.10mL

21.95mL

4.39mL

2.20mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

Historical Records

Categories