BMS-986195 (NWS)

Lub npe tshuaj:

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

SMILES Code:

FC1=C(N2CCCC[C@H](NC(C#CC)=O)C2)C3=C(NC(C)=C3C)C(C(N)=O)=C1

InChi Code:

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

InChi Key:

VJPPLCNBDLZIFG-ZDUSSCGKSA-N

Lo lus tseem ceeb:

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

Solubility:Soluble hauv DMSO

Cia:0 - 4 ° C rau lub sijhawm luv (hnub mus rau lub lis piam), lossis -20 ° C rau lub sijhawm ntev (hli).

Nqe lus piav qhia:

BMS-986195 yog ib tug muaj zog, covalent, irreversible inhibitor ntawm Bruton's tyrosine kinase (BTK), ib tug tswv cuab ntawm Tec tsev neeg ntawm non-receptor tyrosine kinases tseem ceeb hauv antigen-dependent B-cell signaling thiab ua haujlwm. BMS-986195 yog ntau tshaj 5000-fold xaiv rau BTK tshaj tag nrho cov kinases sab nraum Tec tsev neeg, thiab kev xaiv ntawm 9- txog 1010-fold hauv Tec tsev neeg. BMS-986195 inactivated BTK nyob rau hauv tib neeg cov ntshav nrog ib tug ceev tus nqi ntawm inactivation (3.5 × 10-4 nM-1·min-1) thiab potently inhibited antigen-dependent interleukin-6 ntau lawm, CD86 qhia thiab proliferation hauv B hlwb (IC50<1 nM) yam tsis muaj kev cuam tshuam rau kev ntsuas antigen-independent hauv tib lub hlwb.

Hom phiaj: BTK