PRN1008

Ingoa matū:

(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

Waehere 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

Waehere 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

Kī InChi:

LCFFREMLXLZNHE-IEUUHXEXSA-N

Kupumatua:

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

Wairewa:Wairewa i roto i te DMSO

Rokiroki:0 - 4°C mo te wa poto (ra ki nga wiki), -20°C ranei mo te wa roa (marama).

Whakaahuatanga:

Ko te PRN1008 te kaha, te whiriwhiri me te whakakore i te aukati o te BTK ((IC50 = 1.3 ± 0.5 nM).) me nga paanga PD roa i roto i te vivo. Ko te PRN1008 he haumaru, he pai te whakamanawanui i muri i te kotahitanga me te 10 ra te horopeta ki te tangata. Ko te horopeta kia eke ki te > 90% te noho i muri i te horopeta ka hua te noho tuturu me te roa o te noho. Ko te kapinga whainga BTK me te horopeta o ia ra o ≥300mg i eke ki nga taumata rongoa i runga i nga rangahau whakamaoritanga i roto i te tauira kiore o te mate rumati. Ko enei raraunga e tautoko ana i te whanaketanga tonu o PRN1008 hei kaihoko rongoa mo te mate rūmātiki.

Whāinga: BTK