BMS-986195

Orukọ Kemikali:

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

KỌỌDỌ SMILES:

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

Koodu 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

Bọtini InChi:

VJPPLCNBDLZIFG-ZDUSSCGKSA-N

Koko-ọrọ:

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

Solubility:Tiotuka ni DMSO

Ibi ipamọ:0 - 4°C fun igba kukuru (ọjọ si awọn ọsẹ), tabi -20°C fun igba pipẹ (osu).

Apejuwe:

BMS-986195 ti o ni agbara, alamọdaju, inhibitor ti ko ni iyipada ti Bruton's tyrosine kinase (BTK), ọmọ ẹgbẹ ti idile Tec ti awọn kinases tyrosine ti kii ṣe olugba ti o ṣe pataki ni ifihan agbara antigen-ti o gbẹkẹle B-cell ati iṣẹ. BMS-986195 jẹ diẹ sii ju 5000-agbo yiyan fun BTK lori gbogbo kinases ita ti idile Tec, ati selectivity awọn sakani lati 9- si 1010-agbo laarin awọn Tec ebi. BMS-986195 ti ko ṣiṣẹ BTK ninu gbogbo ẹjẹ eniyan pẹlu iyara iyara ti inactivation (3.5 × 10-4 nM-1 · min-1) ati ki o ṣe idiwọ iṣelọpọ antigen-ti o gbẹkẹle interleukin-6, ikosile CD86 ati afikun ninu awọn sẹẹli B (IC50)<1 nM) laisi ipa lori awọn iwọn ominira antijeni ninu awọn sẹẹli kanna.

afojusun: BTK