Ib-847325

Lub npe tshuaj:

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

SMILES Code:

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

InChi Code:

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- 6-5-7-9-2 2) 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-

InChi Key:

FLBNLJLONKAPLR-DQSJHHFOSA-N

Lo lus tseem ceeb:

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

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:

BI-847325 yog ib qho kev xaiv dual MEK / Aurora kinase inhibitor nrog IC50 qhov tseem ceeb ntawm 3, 25, 15, 25, thiab 4 nM rau X. laevis Aurora B, tib neeg Aurora A thiab Aurora C, thiab tib neeg MEK1 thiab MEK2, feem. Nws tuaj yeem cuam tshuam txoj kev loj hlob thiab kev ciaj sia ntawm ob qho tib si kev kho mob-naive thiab tshuaj-resistant melanoma cell kab, txo qhov kev qhia ntawm MEK thiab Mcl-1 thaum nce kev qhia ntawm pro-apoptotic protein Bim. Ntawm 70 mg / kg, BI-847325 induces apoptosis hauv kev kho-naive thiab tshuaj-resistant xenografted melanoma hauv vivo.

Lub Hom Phiaj: MEK / Aurora