I-PRN1008

Igama leMchiza:

(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

Ikhowudi yoncumo:

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

Ikhowudi ye-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

Isitshixo se-InChi:

I-LCFFREMLXLZNHE-IEUUHXEXSA-N

Igama elingundoqo:

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

Ukunyibilika:Inyibilika kwi-DMSO

Ugcino:0 - 4°C ixesha elifutshane (iintsuku ukuya kwiiveki), okanye -20°C ixesha elide (iinyanga).

Inkcazo:

I-PRN1008 yinto enamandla, ekhethiweyo kunye ne-reversible covalent inhibitor ye-BTK ((IC50 = 1.3 ± 0.5 nM)) kunye nemiphumo eyandisiweyo yePD kwi-vivo. I-PRN1008 yayikhuselekile kwaye inyamezeleke emva kokuthatha idosi yosuku olunye kunye ne-10 ebantwini. Ukudongwa ukufikelela> 90% kokuhlala emva kwethamo kukhokelela ekuhlaleni okujoliswe kuko okuhlala ixesha elide. I-BTK ekujoliswe kuyo kunye nedosi yemihla ngemihla ye-≥300mg ifikelele kumanqanaba onyango ngokusekelwe kwizifundo zoguqulo kwimodeli yegundane ye-arthritis. Ezi nkcukacha zixhasa uphuhliso oluqhubekayo lwe-PRN1008 njenge-arhente yonyango ye-rheumatoid arthritis.

Ithagethi: BTK