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Tolebrutinib

CAT: 0804-HY-109192-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-109192-01Size:5 mg
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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].
CAS Number
1971920-73-6
Product Name Alternative
SAR442168; PRN2246
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
Btk
Type
Reference compound
Related Pathways
Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Neurological Disease
Assay Protocol
https://www.medchemexpress.com/tolebrutinib.html
Purity
99.79
Solubility
DMSO : 87.5 mg/mL (ultrasonic)
Smiles
O=C(N1[C@H]2CN(C(C=C)=O)CCC2)N(C3=CC=C(OC4=CC=CC=C4)C=C3)C5=C1C=CN=C5N
Molecular Formula
C26H25N5O3
Molecular Weight
455.51
Precautions
H302, H315, H319, H335
References & Citations
[1]Dahl K, et, al. Radiosynthesis of a Bruton's tyrosine kinase inhibitor, [ 11 C]Tolebrutinib, via palladium-NiXantphos-mediated carbonylation. J Labelled Comp Radiopharm. 2020 Sep;63 (11) :482-487.|[2]Francesco MR, et, al. PRN2246, a potent and selective blood brain barrier penetrating BTK inhibitor, exhibits efficacy in central nervous system immunity. Multiple Sclerosis Journal. 2017; Poster Session 2:P989.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 3

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