Tolebrutinib is an oral, CNS permeable, irreversible BTK inhibitor with IC50 of 0.4 nM and 0.7 nM in Ramos B cells and HMC microglia cells, respectively.

 

Brand: BCM

 

Target: BTK

 

Signaling Pathways: Angiogenesis; Tyrosine Kinase/Adaptors

 

In Vitro: PRN2246 inhibits microglial FcγR activation through durable occupancy of BTK, with an IC50 of 157 nM.?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.

 

Boiling Point: 698.1±65.0 °C(Predicted)

 

pKa: 7.03±0.20(Predicted)

 

Solubility: Soluble in DMSO; Soluble in Ethanol. Insoluble in Water.

 

GHS: GHS07

 

Isomeric 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  

 

InChI: InChI=1S/C26H25N5O3/c1-2-23(32)29-16-6-7-19(17-29)30-22-14-15-28-25(27)24(22)31(26(30)33)18-10-12-21(13-11-18)34-20-8-4-3-5-9-20/h2-5,8-15,19H,1,6-7,16-17H2,(H2,27,28)/t19-/m1/s1

 

Attribute
[Chem Name]	4-amino-3-(4-phenoxyphenyl)-1-[(3R)-1-prop-2-enoylpiperidin-3-yl]imidazo[4,5-c]pyridin-2-one
[Synonym]	Tolebrutinib; SAR442168; PRN2246
[CAS No.]	1971920-73-6
[MDL No.]	MFCD32710277
[Formula]	C26H25N5O3
[Molecular]	455.51
[Form]	Solid Powder
[Storage]	Sealed in dry, 2-8°C

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