I-BMS-986195

Igama Lekhemikhali:

(S)-4-(3-(kodwa-2-ynamido)piperidin-1-yl)-5-fluoro-2,3-dimethyl-1H-indole-7-carboxamide

Ikhodi ye-SMILES:

FC1=C(N2CCC[C@H](NC(C#CC)=O)C2)C3=C(NC(C)=C3C)C(C(N)=O)=C1

Ikhodi ye-InChi:

I-InChI=1S/C20H23FN4O2/c1-4-6-16(26)24-13-7-5-8-25(10-13)19-15(21)9-14(20(22)27)18 -17(19)11(2)12(3)23-18/h9,13,23H,5,7-8,10H2,1-3H3,(H2,22,27)(H,24,26)/ t13-/m0/s1

I-InChi Key:

VJPPLCNBDLZIFG-ZDUSSCGKSA-N

Igama elingukhiye:

BMS-986195, BMS 986195, BMS986195, 1912445-55-6

Ukunyibilika:I-Soluble ku-DMSO

Isitoreji:0 - 4°C isikhathi esifushane (izinsuku ukuya emavikini), noma -20°C isikhathi eside (izinyanga).

Incazelo:

I-BMS-986195 iyisivimbeli esinamandla, esiqinile, esingahlehlakeleki se-Bruton's tyrosine kinase (BTK), ilungu lomndeni wakwa-Tec we-non-receptor tyrosine kinases ebalulekile ekusayineni nasekusebenzeni kwamaseli e-B ancike ku-antigen. I-BMS-986195 ikhetha izikhathi ezingaphezu kuka-5000 ku-BTK phezu kwawo wonke ama-kinases angaphandle komndeni wakwa-Tec, futhi ukukhetha kusuka ku-9- kuya ku-1010-fold phakathi komndeni wakwa-Tec. I-BMS-986195 ingasebenzi i-BTK egazini lonke lomuntu ngezinga elisheshayo lokungasebenzi (3.5×10-4 nM-1·min-1) kanye nokukhiqizwa kwe-interleukin-6 encike ku-antigen, ukuvezwa kwe-CD86 nokwanda kwamaseli B (IC50<1 nM) ngaphandle komphumela ezilinganisweni ezizimele ze-antigen kumaseli afanayo.

Ithagethi: BTK