PRN1008

Inoa Kimia:

(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 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

Code 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

Ki InChi:

LCFFREMLXLZNHE-IEUUHXEXSA-N

huaʻōlelo:

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

Hiki ke hoʻoheheʻe:Hiki ke hoʻoheheʻe ʻia ma DMSO

Waihona:0 - 4°C no ka wā pōkole (nā lā i nā pule), a i ʻole -20°C no ka wā lōʻihi (mau mahina).

wehewehe:

ʻO PRN1008 kahi mea hoʻopaneʻe covalent ikaika, koho a hoʻohuli ʻia o BTK ((IC50 = 1.3 ± 0.5 nM).) me nā hopena PD lōʻihi i vivo. Ua palekana ʻo PRN1008 a ua ʻae maikaʻi ʻia ma hope o ka lā hoʻokahi a me 10 lā dosing i loko o ke kanaka. ʻO ka hoʻopaʻa ʻana no ka loaʻa ʻana o ka 90% noho ma hope o ka hopena o ka hopena o ka noho paʻa ʻana a lōʻihi. ʻO ka uhi paʻa ʻana o BTK me ka nui o kēlā me kēia lā o ≥300mg i hōʻea i nā pae therapeutic e pili ana i nā haʻawina unuhi ma kahi ʻano ʻiole o ka maʻi arthritis. Kākoʻo kēia mau ʻikepili i ka hoʻomau ʻana i ka hoʻomohala ʻana o PRN1008 ma ke ʻano he lāʻau lapaʻau no ka maʻi rheumatoid arthritis.

Pahuhopu: BTK