BI-847325

Orukọ Kemikali:

(Z) -3- (3- (((4- ((dimethylamino)methyl) phenyl) amino) (phenyl) methylene) -2-oxoindolin-6-yl) -N-ethylpropiolamide

KỌỌDỌ SMILES:

O=C(NCC)C#CC1=CC(NC/2=O)=C(C=C1)C2=C(NC3=CC=C(CN(C)C)C=C3)/C4=CC= CC=C4

Koodu InChi:

InChi=1S/C29H28N4O2/c1-4-30-26(34)17-13-20-12-16-24-25(18-20)32-29(35)27(24)28(22-8-) 6-5-7-9-22)31-23-14-10-21 (11-15-23)19-33 (2)3/h5-12,14-16,18,31H,4,19H2, 1-3H3, (H,30,34)(H,32,35)/b28-27-

Bọtini InChi:

FLBNLJLONKAPLR-DQSJHHFOSA-N

Koko-ọrọ:

BI-847325, BI847325, BI 847325, 1207293-36-4

Solubility:Tiotuka ni DMSO

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

Apejuwe:

BI-847325 jẹ oludena meji MEK/Aurora kinase ti o yan pẹlu awọn iye IC50 ti 3, 25, 15, 25, ati 4 nM fun X. laevis Aurora B, eniyan Aurora A ati Aurora C, ati eniyan MEK1 ati MEK2, lẹsẹsẹ. O le ṣe idiwọ idagbasoke ati iwalaaye ti awọn laini sẹẹli melanoma ti o ni itọju ati oogun, dinku ikosile ti MEK ati Mcl-1 lakoko ti o pọ si ikosile ti amuaradagba pro-apoptotic Bim. Ni 70 mg / kg, BI-847325 nfa apoptosis ni itọju-naive ati oogun-sooro xenografted melanoma ni vivo.

Àfojúsùn: MEK/Aurora