醋酸艾塞那肽
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- CAS号:
- 1235034-55-5
- 英文名:
- A-1155463
- 英文别名:
- A-1155463;Exenatide acetate (free base);A-1155463; A 1155463; A1155463.;Bcl-2 Family,Inhibitor,A-1155463,inhibit;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;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;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]-;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
- 中文名:
- 醋酸艾塞那肽
- 中文别名:
- BCL-XL抑制剂(A-1155463);2-(8-(苯并[D]噻唑-2-基胺甲酰基)-3,4-二氢异喹啉-2(1H)-基)-5-(3-(4-(3-(二甲胺基)丙-1-炔-1-基)-2-氟苯氧基)丙基)噻唑-4-甲酸;2-(8-(苯并[D]噻唑-2-基氨基甲酰基)-3,4-二氢异喹啉-2(1H)-基)-5-(3-(4-(3-(二甲基氨基)丙-1-炔 -1-基)-2-氟苯氧基)丙基)噻唑-4-羧酸
- CBNumber:
- CB13066996
- 分子式:
- C35H32FN5O4S2
- 分子量:
- 669.79
- MOL File:
- 1235034-55-5.mol
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醋酸艾塞那肽化学性质
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密度:
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1.45±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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≥67 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
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形态:
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solid
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酸度系数(pKa):
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1.11±0.36(Predicted)
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颜色:
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Off-white to yellow
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醋酸艾塞那肽性质、用途与生产工艺
A-1155463是一种高度有效、选择性的BCL-XL抑制剂。其对BCL-XL的亲和力属于皮摩尔级别,对BCL-2、BCL-W(Ki=19 nM)、MCL-1(Ki>440 nM)的结合比对BCL-XL弱1000倍以上。
Target | Value |
BCL-XL
(Cell-free assay)
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<0.01 nM(Ki)
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A-1155463在细胞中破坏BCL-XL-BIM复合体而不是BCL-2-BIM复合体。A-1155463可以杀死BCL-XL依赖性的Molt-4细胞(IC50=70 nM),但对RS4;11细胞没有明显的细胞毒性(EC50>5 mM)。A-1155463在BCL-XL依赖性的H146细胞中诱导凋亡标志,如线粒体释放细胞色素c、caspase的激活、caspase依赖性的sub-G0-G1期DNA的含量积累。
向SCID-Beige不带瘤小鼠中单次腹腔注射5 mg/kg A-1155463,血小板数量在注射后6小时显著下降,在注射后72小时内恢复为正常水平。每天向接种过BCL-XL依赖性H146肿瘤细胞的SCID-Beige小鼠腹腔注射5 mg/kg A-1155463,14天后检测,A-1155463显著抑制了肿瘤的生长,在停止给药后,效果减轻。
醋酸艾塞那肽
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/08/19 | HY-19725 | A-1155463 | | 1 mg | 571元 |
2024/08/19 | HY-19725 | 醋酸艾塞那肽 A-1155463 | 1235034-55-5 | 2mg | 850元 |
1235034-55-5, 醋酸艾塞那肽 相关搜索:
- 标准品
- 细胞生物学试剂
- C35H32FN5O4S2
- 2-(8-(苯并[D]噻唑-2-基胺甲酰基)-3,4-二氢异喹啉-2(1H)-基)-5-(3-(4-(3-(二甲胺基)丙-1-炔-1-基)-2-氟苯氧基)丙基)噻唑-4-甲酸
- 2-(8-(苯并[D]噻唑-2-基氨基甲酰基)-3,4-二氢异喹啉-2(1H)-基)-5-(3-(4-(3-(二甲基氨基)丙-1-炔 -1-基)-2-氟苯氧基)丙基)噻唑-4-羧酸
- BCL-XL抑制剂(A-1155463)
- 1235034-55-5
- Exenatide acetate (free base)
- Bcl-2 Family,Inhibitor,A-1155463,inhibit
- 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
- 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]-
- A-1155463; A 1155463; A1155463.
- 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
- 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
- A-1155463