A-1155463
Modify Date: 2024-01-10 10:48:27
A-1155463 structure
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Common Name | A-1155463 | ||
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| CAS Number | 1235034-55-5 | Molecular Weight | 669.788 | |
| Density | 1.5±0.1 g/cm3 | Boiling Point | N/A | |
| Molecular Formula | C35H32FN5O4S2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of A-1155463A-1155463 is a highly potent and selective BCL-XL inhibitor with an EC50 of 70 nM in Molt-4 cell. |
| Name | 2-[8-(1,3-Benzothiazol-2-ylcarbamoyl)-3,4-dihydro-2(1H)-isoquinolinyl]-5-(3-{4-[3-(dimethylamino)-1-propyn-1-yl]-2-fluorophenoxy}propyl)-1,3-thiazole-4-carboxylic acid |
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| Synonym | More Synonyms |
| Description | A-1155463 is a highly potent and selective BCL-XL inhibitor with an EC50 of 70 nM in Molt-4 cell. |
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| Related Catalog | |
| Target |
Bcl-xL:0.01 nM (Ki) Bcl-2:80 nM (Ki) |
| 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]. |
| In Vivo | A-1155463 caused a mechanism-based and reversible thrombocytopenia in mice and inhibited H146 small cell lung cancer xenograft tumor growth in vivo following multiple doses[2]. |
| Animal Admin | Mice: Following a single 5 mg/kg IP dose of A-1155463 in nontumor bearing SCID-Beige mice, platelet counts fell dramatically as measured at 6 h postdose and then rebounded to normal levels within 72 h. A-1155463 is then administered to SCID-Beige mice that had been inoculated with BCL-XL-dependent H146 tumor cells with a daily dose at 5 mg/kg IP for 14 days[2]. |
| References |
| Density | 1.5±0.1 g/cm3 |
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| Molecular Formula | C35H32FN5O4S2 |
| Molecular Weight | 669.788 |
| Exact Mass | 669.187988 |
| LogP | 6.61 |
| Index of Refraction | 1.716 |
| Storage condition | -20℃ |
| 2-[8-(1,3-Benzothiazol-2-ylcarbamoyl)-3,4-dihydro-2(1H)-isoquinolinyl]-5-(3-{4-[3-(dimethylamino)-1-propyn-1-yl]-2-fluorophenoxy}propyl)-1,3-thiazole-4-carboxylic acid |
| 4-Thiazolecarboxylic acid, 2-[8-[(2-benzothiazolylamino)carbonyl]-3,4-dihydro-2(1H)-isoquinolinyl]-5-[3-[4-[3-(dimethylamino)-1-propyn-1-yl]-2-fluorophenoxy]propyl]- |
| A1155463 |
| A-1155463 |