Mtengo wa PRN1008

Dzina la Chemical:

(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 Kodi:

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 kodi:

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:

Chithunzi cha LCFFREMLXLZNHE-IEUUHXEXSA-N

Mawu ofunika:

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

Kusungunuka:Zosungunuka mu DMSO

Posungira:0 - 4 ° C kwa nthawi yochepa (masiku mpaka masabata), kapena -20 ° C kwa nthawi yaitali (miyezi).

Kufotokozera:

PRN1008 ndi yamphamvu, yosankha komanso yosinthika covalent inhibitor ya BTK ((IC50 = 1.3 ± 0.5 nM).) yokhala ndi zotsatira zowonjezera za PD mu vivo. PRN1008 inali yotetezeka komanso yololera pambuyo pa kumwa limodzi ndi masiku 10 mwa anthu. Mlingo kuti mukwaniritse> 90% wokhalamo mutalandira mlingo kumabweretsa kukhalapo kwanthawi zonse komanso kwanthawi yayitali. BTK chandamale chandamale ndi mlingo watsiku ndi tsiku wa ≥300mg chinafika pamiyezo yochizira kutengera maphunziro omasulira amtundu wa makoswe a nyamakazi. Izi zimathandizira kupititsa patsogolo chitukuko cha PRN1008 monga chithandizo chamankhwala a nyamakazi ya nyamakazi.

Cholinga: BTK