PRN1008

Lub npe tshuaj:

(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-enitrile

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

Lo lus tseem ceeb:

PRN 1008, PRN-1008, PRN 1008, 1575596-29-0, PAB

Solubility:Soluble hauv DMSO

Cia:0 - 4 ° C rau lub sijhawm luv (hnub mus rau lub lis piam), lossis -20 ° C rau lub sijhawm ntev (hli).

Nqe lus piav qhia:

PRN1008 yog lub zog, xaiv thiab thim rov qab covalent inhibitor ntawm BTK ((IC50 = 1.3 ± 0.5 nM).) nrog txuas ntxiv PD teebmeem hauv vivo. PRN1008 muaj kev nyab xeeb thiab zam tau zoo tom qab noj ib zaug thiab 10 hnub rau tib neeg. Kev noj tshuaj kom ua tiav> 90% nyob tom qab noj tshuaj ua rau muaj kev sib luag thiab ntev lub hom phiaj. BTK lub hom phiaj kev pab cuam nrog ib koob tshuaj txhua hnub ntawm ≥300mg mus txog qib kho raws li kev tshawb fawb kev txhais lus hauv tus qauv nas ntawm kev mob caj dab. Cov ntaub ntawv no txhawb kev txhim kho txuas ntxiv ntawm PRN1008 ua tus neeg sawv cev kho mob rau rheumatoid mob caj dab.

Hom phiaj: BTK