PRN1008

Magaca Kiimikada:

(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) pent-2-enenitrile

Koodhka dhoola cadeynta:

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

Koodhka 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

Furaha InChi:

LCFFREMLXLZNHE-IEUUHXEXSA-N

Ereyga muhiimka ah:

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

Xalka:Ku milmay DMSO

Kaydinta:0 - 4°C muddo gaaban (maalmo ilaa toddobaadyo), ama -20°C muddo dheer (bilo).

Sharaxaad:

PRN1008 waa mid awood leh, la xushay oo dib loo celin karo xannibaadaha BTK ((IC50 = 1.3 ± 0.5 nM)). PRN1008 waxay ahayd badbaado oo si wanaagsan loo dulqaatay ka dib markii hal iyo 10 maalmood la qaatay qiyaasta bini'aadamka. Qaadashada si loo gaadho> 90% degenaansho ka dib qiyaasta waxay keentaa degenaansho joogto ah oo daba dheeraada. Caymiska bartilmaameedka BTK oo leh qiyaasta maalinlaha ah ee ≥300mg ayaa gaadhay heerar daweyn oo ku salaysan daraasado tarjumaad ah oo ah qaabka jiirka ee arthritis-ka. Xogtaasi waxay taageertaa horumarinta joogtada ah ee PRN1008 sida wakiilka daweynta ee rheumatoid arthritis-ka.

Ujeedka: BTK