PRN1008

Non Chimik:

(S)-2-(3-(4-amino-3-(2-fluoro-4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pirimidin-1-yl)piperidin-1-carbonyl)-4 -methyl-4-(4-(oksetan-3-yl)piperazin-1-yl)pent-2-enenitrile

Kòd SMILES:

NC1=C2C(N([C@H]3CCCN(C(/C(C#N))=CC(C))(N4CCN(C5COC5)CC4)C)=O)C3)N=C2C6=C(F)C =C(OC7=CC=CC=C7)C=C6)=NC=N1

Kòd InChi:

InChI=1S/C36H40FN9O3/c1-36(2,45-15-13-43(14-16-45)26-21-48-22-26)18-24(19-38)35(47)44- 12-6-7-25(20-44)46-34-31(33(39)40-23-41-34)32(42-46)29-11-10-28(17-30(29) 37)49-27-8-4-3-5-9-27/h3-5,8-11,17-18,23,25-26H,6-7,12-16,20-22H2,1- 2H3,(H2,39,40,41)/b24-18-/t25-/m0/s1

InChi kle:

LCFFREMLXLZNHE-IEUUHXEXSA-N

Mot:

PRN1008, PRN-1008, PRN 1008,1575596-29-0

Solibilite:Soluble nan DMSO

Depo:0 - 4 ° C pou kout tèm (jou a semèn), oswa -20 ° C pou tèm long (mwa).

Deskripsyon:

PRN1008 se yon inhibitor kovalan ki pisan, selektif ak revèsib nan BTK ((IC50 = 1.3 ± 0.5 nM).) ak efè PD pwolonje nan vivo. PRN1008 te an sekirite ak byen tolere apre yon sèl ak 10 jou dòz nan imen. Dòz pou reyalize > 90% lokatè apre yon dòz rezilta nan lokatè sib ki konsistan ak pwolonje. Kouvèti sib BTK ak yon dòz chak jou nan ≥300mg rive nan nivo terapetik ki baze sou syans tradiksyon nan yon modèl rat nan atrit. Done sa yo sipòte devlopman kontinye nan PRN1008 kòm yon ajan terapetik pou atrit rimatoyid.

Sib: BTK