BMS-986195

Ingoa matū:

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

Waehere SMILES:

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

Waehere InChi:

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

Kī InChi:

VJPPLCNBDLZIFG-ZDUSSCGKSA-N

Kupumatua:

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

Wairewa:Wairewa i roto i te DMSO

Rokiroki:0 - 4°C mo te wa poto (ra ki nga wiki), -20°C ranei mo te wa roa (marama).

Whakaahuatanga:

Ko te BMS-986195 he kaha, he kovalent, he aukati korekore o te tyrosine kinase (BTK) a Bruton, he mema o te whanau Tec o nga kinases tyrosine kore-receptor e tino nui ana i roto i te tohu tohu-a-antigen-tiakitanga me te mahi. Ko te BMS-986195 neke atu i te 5000-fold te whiriwhiringa mo te BTK i runga i nga kinase katoa i waho o te whanau Tec, me te awhe mai i te 9- ki te 1010-fold i roto i te whanau Tec. Ko te BMS-986195 i whakakorehia te BTK i roto i te toto katoa o te tangata me te tere tere o te whakakore (3.5 × 10-4 nM-1 · min-1) me te kaha te aukati i te hanga interleukin-6 e whakawhirinaki ana ki te antigen, te whakaaturanga CD86 me te tipu i roto i nga kamera B (IC50).<1 nM) karekau he painga ki nga inenga motuhake-antigen i roto i nga ruma kotahi.

Whāinga: BTK