BiochemProbe — Life Science Research Reagents

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.

Purity >98% Stock Inquire

Tolebrutinib structure

CAS No.: 1971920-73-6

Download structure (.mol)

Pack sizes & pricing

Size Price SKU Stock
250 mg USD 485.00 BP-01956-250mg In stock Get quote
500 mg USD 785.00 BP-01956-500mg In stock Get quote
1 g USD 1,250.00 BP-01956-1g In stock Get quote
5 g Inquire BP-01956-5g Inquire Inquire

Need another size or custom synthesis? Request a quote.

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

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.

Same target

Search Btk

Same research area

Search Neurological Disease

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