A-1155463
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Ki = 19 nM
A-1155463是一种强效的和选择性的BCL-XL抑制剂。
BCL-2在淋巴恶性肿瘤的存活中起关键作用，而BCL-XL过表达与各种实体瘤和血液恶性肿瘤的耐药性和疾病进展相关。
体外：通过核磁共振片段筛选和基于结构的设计，鉴定A-1155463为一种高效的和选择性的BCL-XL抑制剂。相对于先前报道的抑制剂WEHI-539，A-1155463对BCL-XL依赖性细胞系显著更有效[1]。
体内：动物研究显示，在非肿瘤载有SCID-Beige小鼠中，单次腹腔注射5 mg/kg的A-1155463后，在给药后6小时血小板计数显著降低，然后在72小时内回复至正常水平。这种血小板消耗和恢复动力学类似于双重抑制剂navitoclax。此外，为了给出A-1155463靶向体内活性的额外证据，对已接种BCL-XL依赖性H146肿瘤细胞的SCIDBeige小鼠给药。结果显示，5 mg / kg日剂量的A-1155463 腹腔给药14天导致肿瘤生长的统计学显著抑制，且在停药后缓解[1]。
临床试验：到目前为止，A-1155463仍处于临床前研究阶段。
参考文献：
[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.
- 1. Rana Estaleen. "Characterizing Senescence Induction and Senolytic Sensitivity in Murine Lung Cancer Cell Lines." Virginia Commonwealth University. May 10, 2022.
- 2. Anna L. Koessinger, Catherine Cloix, et al. "Increased apoptotic sensitivity of glioblastoma enables therapeutic targeting by BH3-mimetics." Cell Death Differ. 2022 Apr 26. PMID: 35473984
- 3. Constanze Kurschat, Arlena Metz, et al. "Importance of Bcl-2-family proteins in murine hematopoietic progenitor and early B cells." Cell Death Dis. 2021 Aug 11;12(8):784. PMID: 34381022
- 4. Rago F, DiMare MT, et al. "Degron mediated BRM/SMARCA2 depletion uncovers novel combination partners for treatment of BRG1/SMARCA4-mutant cancers." Biochem Biophys Res Commun. 2019 Jan 1;508(1):109-116. PMID: 30527810
- 5. Wilson Xuan Mai."Comprehensive Characterization of the Apoptotic Machinery in Glioblastoma Identifies New Therapeutic Strategies." UNIVERSITY OF CALIFORNIA. 2018-01-01.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 669.79 |
| Cas No. | 1235034-55-5 |
| Formula | C35H32FN5O4S2 |
| Solubility | ≥67 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
| Chemical Name | 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 |
| SDF | Download SDF |
| 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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
质量控制和MSDS
- 批次:
化学结构
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