PRN1008

Orukọ Kemikali:

(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

KỌỌDỌ 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

Koodu 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

Bọtini InChi:

LCFFREMLXLZNHE-IEUUHXEXSA-N

Koko-ọrọ:

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

Solubility:Tiotuka ni DMSO

Ibi ipamọ:0 - 4°C fun igba kukuru (ọjọ si awọn ọsẹ), tabi -20°C fun igba pipẹ (osu).

Apejuwe:

PRN1008 jẹ agbara, yiyan ati oludaniloju covalent ti BTK ((IC50 = 1.3 ± 0.5 nM)) pẹlu awọn ipa PD ti o gbooro ni vivo. PRN1008 jẹ ailewu ati ifarada daradara lẹhin iwọn ẹyọkan ati ọjọ mẹwa 10 ninu eniyan. Ṣiṣe iwọn lilo lati ṣaṣeyọri> 90% ibugbe lẹhin awọn abajade iwọn lilo ni deede ati igbaduro ibi-afẹde gigun. Agbegbe ibi-afẹde BTK pẹlu iwọn lilo ojoojumọ ti ≥300mg ti de awọn ipele itọju ailera ti o da lori awọn ikẹkọ itumọ ni awoṣe eku ti arthritis. Awọn data wọnyi ṣe atilẹyin idagbasoke idagbasoke ti PRN1008 gẹgẹbi oluranlowo itọju ailera fun arthritis rheumatoid.

afojusun: BTK