PRN1008

Izina ryimiti:

(S) -2- (3- (4-amino-3- (2-fluoro-4-phenoxyphenyl) -1H-pyrazolo -methyl-4- (4- (oxetan-3-yl) piperazin-1-yl) pent-2-enenitrile

Kode ya 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

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 Urufunguzo:

LCFFREMLXLZNHE-IEUUHXEXSA-N

Ijambo ryibanze:

PRN1008, PRN-1008, PRN 1008.1575596-29-0

Gukemura:Gukemura muri DMSO

Ububiko:0 - 4 ° C mugihe gito (iminsi kugeza ibyumweru), cyangwa -20 ° C mugihe kirekire (amezi).

Ibisobanuro:

PRN1008 nimbaraga zikomeye, zitoranya kandi zishobora guhindurwa covalent inhibitor ya BTK ((IC50 = 1.3 ± 0.5 nM).) Hamwe n'ingaruka za PD zagutse muri vivo. PRN1008 yari ifite umutekano kandi yihanganirwa nyuma yumunsi umwe niminsi 10 mu bantu. Gukoresha kugirango ugere kuri> 90% gutura nyuma yikinini gisubizo muburyo buhoraho kandi burigihe. Intego ya BTK hamwe na dose ya buri munsi ya 00300mg yageze kurwego rwo kuvura rushingiye kubushakashatsi bwubuhinduzi muburyo bwimbeba ya rubagimpande. Aya makuru ashyigikira gukomeza iterambere rya PRN1008 nkumuti wo kuvura rubagimpande ya rubagimpande.

Intego: BTK