PRN1008

Nomen chemicum:

(S)-2-(3-(4-amino-3-(2-fluoro-4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carbonyl)-4 -methyl-4-(4-(oxetan-3-yl)piperazin-1-yl) inclusus-2-enenitrile

SMILES Code:

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

InChi Code:

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)49-278-4-3-5-9-27/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 Key:

LCFFREMLXLZNHE-IEUUHXEXSA-N

Keyword:

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

Solubilitas:Solutum in DMSO

Repono:0 - 4°C ad terminum brevem (dies ad septimanas), vel -20°C ad terminum longi (menses).

Descriptio:

PRN1008 inhibitor covalentis inhibitoris BTK potentis, selectivi et convertibilis est (IC50 = 1.3 ± 0,5 nM).) productis PD effectibus vivo. PRN1008 tuta et bene tolerata fuit post singulos et 10 dies dosing in hominibus. Dosing ad consequi> XC% negotium post dose praecessi in constantem et longum scopum negotium. BTK scopum coverage cum cotidiano pondere ≥300mg pervenit ad gradus therapeuticos fundatus in studiis translationalibus in exemplari arthritis ratti. Haec data subsidia continuam progressionem PRN1008 tamquam agentis therapeuticae pro arthritis rheumatoideis.

Target: BTK