PRN1008

Chemical Name:

(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 Kodhi:

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

Keyword:

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

Solubility:Soluble muDMSO

Kuchengeta:0 - 4 ° C kwenguva pfupi (mazuva kusvika mavhiki), kana -20 ° C kwenguva refu (mwedzi).

Tsanangudzo:

PRN1008 ine simba, inosarudza uye inodzoreredzwa covalent inhibitor yeBTK ((IC50 = 1.3 ± 0.5 nM).) ine yakawedzera PD mhedzisiro mu vivo. PRN1008 yaive yakachengeteka uye yakatenderwa zvakanaka mushure mekusaroorwa uye 10 zuva dosing muvanhu. Dosing yekuwana> 90% yekugara mushure meiyo dosi inoguma nekuenderana uye kwenguva refu kwechinangwa chekugara. BTK yakananga kufukidzwa nedosi yezuva nezuva ye ≥300mg yakasvika nhanho dzekurapa zvichibva pazvidzidzo zveshanduro mumuenzaniso wemakonzo earthritis. Iyi data inotsigira kuenderera mberi kwePRN1008 semushonga wekurapa rheumatoid arthritis.

Chinangwa: BTK