Cas No.: | 1235034-55-5 |
Chemical Name: | A-1155463 |
Synonyms: | A-1155463;A1155463;2-[8-(1,3-Benzothiazol-2-Ylcarbamoyl)-3,4-Dihydroisoquinolin-2(1h)-Yl]-5-(3-{4-[3-(Dimethylamino)prop-1-Yn-1-Yl]-2-Fluorophenoxy}propyl)-1,3-Thiazole-4-Carboxylic Acid;2-(8-(benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1H)-yl)-5-(3-(4-(3-(dimethylamino)prop-1-yn-1-yl)-2-fluorophenoxy)propyl)thiazole-4-carboxylic acid;2-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-5-[3-[4-[3-(dimethylamino)prop-1-ynyl]-2-fluorophenox |
SMILES: | S1C(=C(C(=O)O)N=C1N1CC2C(C(NC3=NC4=CC=CC=C4S3)=O)=CC=CC=2CC1)CCCOC1C=CC(C#CCN(C)C)=CC=1F |
Formula: | C35H32FN5O4S2 |
M.Wt: | 669.7881 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | A-1155463 is a highly potent and selective BCL-XL inhibitor with an EC50 of 70 nM in Molt-4 cell. |
In Vivo: | A-1155463 shows picomolar binding affinity to BCL-XL (Ki<0.01 nM), and >1000-fold weaker binding to BCL-2 (Ki= 80 nM) and related proteins BCL-W (Ki= 19 nM) and MCL-1 (Ki> 440 nM) [2]. A-1155463 demonstrates strong growth inhibition of over half of the colorectal cell lines as defined by EC50 values ≤0.5 μM in the presence of 10 % FBS[3]. |
In Vitro: | A-1155463 shows picomolar binding affinity to BCL-XL (Ki<0.01 nM), and >1000-fold weaker binding to BCL-2 (Ki= 80 nM) and related proteins BCL-W (Ki= 19 nM) and MCL-1 (Ki> 440 nM) [2]. A-1155463 demonstrates strong growth inhibition of over half of the colorectal cell lines as defined by EC50 values ≤0.5 μM in the presence of 10 % FBS[3]. |