1. Protein Tyrosine Kinase/RTK
  2. Btk
  3. Tolebrutinib

Tolebrutinib (Synonyms: SAR442168; PRN2246)

Cat. No.: HY-109192 Purity: 98.96%
Handling Instructions

Tolebrutinib (SAR442168) is a potent, selective, orally active and brain-penetrant inhibitor of Bruton tyrosine kinase (BTK), with IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively. Tolebrutinib exhibits efficacy in central nervous system immunity. Tolebrutinib can be used for the research of multiple sclerosis (MS).

For research use only. We do not sell to patients.

Tolebrutinib Chemical Structure

Tolebrutinib Chemical Structure

CAS No. : 1971920-73-6

Size Price Stock Quantity
5 mg USD 400 In-stock
Estimated Time of Arrival: December 31
10 mg USD 680 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1950 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2900 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Tolebrutinib (SAR442168) is a potent, selective, orally active and brain-penetrant inhibitor of Bruton tyrosine kinase (BTK), with IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively. Tolebrutinib exhibits efficacy in central nervous system immunity. Tolebrutinib can be used for the research of multiple sclerosis (MS)[1][2].

IC50 & Target

IC50: 0.7 nM (BTK; in HMC microglia cells)[2]

In Vitro

PRN2246 blocks the BCR-mediated activation (IC50=10 nM) and Fc receptor activation (IC50=166 and 9.6 nM for FcεR and FcγR, repectively) of immune cells[2].
PRN2246 inhibits microglial FcγR activation through durable occupancy of BTK, with an IC50 of 157 nM[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PRN2246 (1-5 mg/kg; p.o. q.d. for 28 d) produces dose-dependent protection from in myelin oligodendrocyte glycoprotein (MOG)-induced experimental autoimmune encephalomyelitis (EAE) model[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

455.51

Formula

C₂₆H₂₅N₅O₃

CAS No.

1971920-73-6

SMILES

O=C(N1[[email protected]]2CN(C(C=C)=O)CCC2)N(C3=CC=C(OC4=CC=CC=C4)C=C3)C5=C1C=CN=C5N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (219.53 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1953 mL 10.9767 mL 21.9534 mL
5 mM 0.4391 mL 2.1953 mL 4.3907 mL
10 mM 0.2195 mL 1.0977 mL 2.1953 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

TolebrutinibSAR442168 PRN2246SAR 442168SAR-442168PRN2246PRN 2246PRN-2246BtkBruton tyrosine kinaseBrutontyrosinekinaseBTKmultiplesclerosisMSInhibitorinhibitorinhibit

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Tolebrutinib
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HY-109192
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