PRN1008

Lebitso la lik'hemik'hale:

(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 Khouto:

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

Khoutu ea 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

InChi Key:

LCFFREMLXLZNHE-IEUUHXEXSA-N

Keyword:

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

Sollubility:E qhibiliha ka DMSO

Polokelo:0 - 4 ° C bakeng sa nako e khutšoanyane (matsatsi ho isa libeke), kapa -20 ° C bakeng sa nako e telele (likhoeli).

Tlhaloso:

PRN1008 ke covalent inhibitor e matla, e khethang le e fetohang ea BTK ((IC50 = 1.3 ± 0.5 nM)) e nang le liphello tse atolositsoeng tsa PD ho vivo. PRN1008 e ne e bolokehile 'me e mamelloa hantle ka mor'a ho noa motho a le mong le matsatsi a 10. Ho noa ho fihlela ho lula ho> 90% ka mor'a tekanyetso ho fella ka ho lula hoa nako e telele. Tšireletso ea BTK e nang le tekanyo ea letsatsi le letsatsi ea ≥300mg e fihlile maemong a phekolo e thehiloeng lithutong tsa phetolelo ho mohlala oa rat ea ramatiki. Ts'ehetso ena ea data e tsoelang pele nts'etsopele ea PRN1008 e le moemeli oa phekolo bakeng sa ramatiki ea ramatiki.

Sepheo: BTK