2-(8-(benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1H)-yl)-5-(3-(4-(3-(dimethylamino)prop-1-ynyl)-2-fluorophenoxy)propyl)thiazole-4-carboxylic acid
A-1155463
CAS: 1235034-55-5
Molecular Formula: C35H32FN5O4S2
2-(8-(benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1H)-yl)-5-(3-(4-(3-(dimethylamino)prop-1-ynyl)-2-fluorophenoxy)propyl)thiazole-4-carboxylic acid - Names and Identifiers
2-(8-(benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1H)-yl)-5-(3-(4-(3-(dimethylamino)prop-1-ynyl)-2-fluorophenoxy)propyl)thiazole-4-carboxylic acid - Physico-chemical Properties
| Molecular Formula | C35H32FN5O4S2 |
| Molar Mass | 669.79 |
| Density | 1.45±0.1 g/cm3(Predicted) |
| Solubility | DMSO: ≥ 31 mg/mL |
| pKa | 1.11±0.36(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | A- 1155463 disrupts the BCL-XL-BIM complex but not the BCL-2-BIM complex in the cell. A- 1155463 could kill BCL-XL-dependent Molt-4 cells (IC50=70 nM), but showed no significant cytotoxicity to RS4;11 cells (EC50>5 mM). A- 1155463 induced apoptosis markers in BCL-XL-dependent H146 cells, such as mitochondrial release of cytochrome c, caspase activation, and caspase-dependent sub-G0-G1-phase DNA content accumulation. |
| In vivo study | After A single intraperitoneal injection of 5 mg/kg A- 1155463 into SCID-Beige tumor-free mice, the number of platelets decreased significantly at 6 hours after injection and returned to normal levels within 72 hours after injection. SCID-Beige mice inoculated with BCL-XL-dependent H146 tumor cells were intraperitoneally injected with 5 mg/kg A- 1155463 every day. After 14 days, the A- 1155463 significantly inhibited the growth of tumors, the effect is reduced. |
2-(8-(benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1H)-yl)-5-(3-(4-(3-(dimethylamino)prop-1-ynyl)-2-fluorophenoxy)propyl)thiazole-4-carboxylic acid - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.493 ml | 7.465 ml | 14.93 ml |
| 5 mM | 0.299 ml | 1.493 ml | 2.986 ml |
| 10 mM | 0.149 ml | 0.747 ml | 1.493 ml |
| 5 mM | 0.03 ml | 0.149 ml | 0.299 ml |
Last Update：2024-01-02 23:10:35
2-(8-(benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1H)-yl)-5-(3-(4-(3-(dimethylamino)prop-1-ynyl)-2-fluorophenoxy)propyl)thiazole-4-carboxylic acid - Reference Information
| biological activity | A-1155463 is a highly potent and selective BCL-XL inhibitor. Its affinity for BCL-XL is of the picomolar order, and its binding for BCL-2, BCL-W(Ki = 19 nM), MCL-1(Ki>440 nM) is more than 1000 times weaker than BCL-XL. |
| Target | Value |
| BCL-XL (Cell-free assay) | <0.01 nM(Ki) |
Last Update：2024-04-09 20:49:11
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Product Name: A-1155463 Visit Supplier Webpage Request for quotation
CAS: 1235034-55-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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CAS: 1235034-55-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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