PRN1008

Igoa vaila'au:

(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

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)49-27-8-4-3-5-9-27/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 Key:

LCFFREMLXLZNHE-IEUUHXEXSA-N

upu autu:

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

Solubility:Solu i le DMSO

Teuina:0 - 4°C mo taimi pupuu (aso i vaiaso), poo le -20°C mo taimi uumi (masina).

Fa'amatalaga:

PRN1008 o se inhibitor covalent malosi, filifili ma toe faʻafoʻiina o le BTK ((IC50 = 1.3 ± 0.5 nM).) Faʻatasi ai ma aʻafiaga PD faʻalautele i vivo. O le PRN1008 sa saogalemu ma fa'amalie lelei pe a uma le tu'ufua tasi ma le 10 aso i tagata. Tu'u ina ia ausia > 90% nofoia pe a mae'a se tui e maua ai le tumau ma fa'aumi le nofoia. BTK fa'amoemoega fa'atatau ile fua ole aso ole ≥300mg na o'o ile maualuga ole togafitiga fa'avae ile su'esu'ega fa'aliliuga ile fa'ata'ita'iga o isumu ole gasegase. O nei fa'amaumauga e lagolagoina le fa'aauauina o le atina'eina o le PRN1008 e avea o se vaila'au fa'afoma'i mo fa'ama'i rūmatoid.

Sini: BTK