Tolebrutinib free base · Synonyms: SAR442168 | PRN2246
Tolebrutinib is a potent, selective and brain-penetrant BTK inhibitor.
For research use only. Not for human or veterinary use.
Target
Btk
Purity >98%
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Tolebrutinib structure
CAS No.: 1971920-73-6
Pack sizes & pricing
Description
Tolebrutinib (SAR442168) is a potent, selective and brain-penetrant BTK inhibitor, with IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively.
Biological activity
Tolebrutinib (SAR442168, PRN2246) is a potent, selective 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.
Identifiers
- SMILES
-
C=CC(=O)N1CCC[C@H](C1)N2C3=C(C(=NC=C3)N)N(C2=O)C4=CC=C(C=C4)OC5=CC=CC=C5 - InChIKey
-
KOEUOFPEZFUWRF-LJQANCHMSA-N
Specifications
- MW (average)
- 455.5084
- Formula
- C26H25N5O3
- CAS No.
- 1971920-73-6
- Physical state
- Solid
- Color
- Off-white to light yellow
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Powder -20℃ 2 years; In solvent -20℃ 1 month;
Solubility
Soluble in DMSO
Documents
References
[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.