A-1155463
(Synonyms: 醋酸艾塞那肽) 目录号 : GC17512
A Bcl-xL inhibitor
Cas No.:1235034-55-5
Sample solution is provided at 25 µL, 10mM.
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Ki=19 nM
A-1155463 is a potent and selective BCL-XL inhibitor.
BCL-2 plays a key role in the survival of lymphoid malignancies, while BCL-XL overexpression has been associated with drug resistance and disease progression of various solid tumors and hematological malignancies.
In vitro: A-1155463 was identified via nuclear magnetic resonance fragment screening and structure-based design to be a highly potent and selective BCL-XL inhibitor. A-1155463 was found to be substantially more potent against BCL-XL-dependent cell lines relative to the previously reported inhibitor, WEHI-539 [1].
In vivo: Animal study showed that following a single IP dose of A-1155463 at 5 mg/kg in nontumor bearing SCID-Beige mice, platelet counts dramatically decreased at 6 h postdose and then rebounded to normal levels within 72 h. Such platelet depletion and recovery kinetics were similar to those of the dual inhibitor navitoclax. Moreover, in order to give additional evidence that A-1155463 was conferring on-target in-vivo activity, A-1155463 was then administered to SCIDBeige mice that had been inoculated with BCL-XL-dependent H146 tumor cells. Results showed that the daily IP dosing of A-1155463 at 5 mg/kg for 14 days caused a statistically significant inhibition of tumor growth, which was alleviated upon cessation of dosing [1].
Clinical trial: Up to now, A-1155463 is still in the preclinical development stage.
Reference:
[1] Tao ZF et al. Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity. ACS Med Chem Lett. 2014 Aug 26;5(10):1088-93.
Animal experiment: | 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: [1]. Leverson JD, et al. Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy. Sci Transl Med. 2015 Mar 18;7(279):279 | |
| Cas No. | 1235034-55-5 | SDF | |
| 别名 | 醋酸艾塞那肽 | ||
| 化学名 | 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 | ||
| Canonical SMILES | O=C(C1=C(CCCOC2=CC=C(C#CCN(C)C)C=C2F)SC(N3CC4=C(C=CC=C4C(NC5=NC6=CC=CC=C6S5)=O)CC3)=N1)O | ||
| 分子式 | C35H32FN5O4S2 | 分子量 | 669.79 |
| 溶解度 | ≥ 67mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.493 mL | 7.465 mL | 14.9301 mL |
| 5 mM | 0.2986 mL | 1.493 mL | 2.986 mL |
| 10 mM | 0.1493 mL | 0.7465 mL | 1.493 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet