ABT-263 (Navitoclax)
Catalog No.
A3007
Bcl-2家族抑制剂，可以抑制Bcl-2、 Bcl-xL和Bcl-w。
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ABT-263是一种可口服的选择性Bcl-2家族小分子抑制剂，具有潜在的抗肿瘤活性。其分子式为C47H55ClF3N5O6S3，分子量为974。ABT-263与Bcl-2家族蛋白Bcl-2、Bcl-xl和Bcl-w相结合，干扰Bcl-2/Bcl-xl /Bcl-w与促凋亡蛋白Bim、Bad 和Bak的相互作用，从而启动caspases介导的细胞死亡途径，诱导细胞凋亡。
参考文献：
1. Tse et al., ABT-263: A Potent and Orally Bioavailable Bcl-2 Family Inhibitor. Cancer Res. 2008, 68, 3421-3428.
2. Shoemaker et al., Activity of the Bcl-2 Family Inhibitor ABT-263 in a Panel of Small Cell Lung Cancer Xenograft Models. Clin. Cancer Res. 2008, 14, 3268-3277
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| Storage | Desiccate at -20°C |
| M.Wt | 974.61 |
| Cas No. | 923564-51-6 |
| Formula | C47H55ClF3N5O6S3 |
| Synonyms | Navitoclax,ABT-263,ABT263,ABT 263 |
| Solubility | ≥48.73 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
| Chemical Name | (R)-4-(4-((4'-chloro-4,4-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)-N-((4-((4-morpholino-1-(phenylthio)butan-2-yl)amino)-3-((trifluoromethyl)sulfonyl)phenyl)sulfonyl)benzamide |
| SDF | Download SDF |
| Canonical SMILES | CC(CC1)(C)CC(CN2CCN(C3=CC=C(C(NS(C4=CC=C(N[C@@H](CSC5=CC=CC=C5)CCN6CCOCC6)C(S(C(F)(F)F)(=O)=O)=C4)(=O)=O)=O)C=C3)CC2)=C1C7=CC=C(Cl)C=C7 |
| 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。 |
| 细胞实验[1]： | |
|
细胞系 |
表达小鼠Bcl-2、Bcl-xL和Bcl-w蛋白的小鼠DO11.10 T杂交瘤细胞 |
|
溶解方法 |
在DMSO中的溶解度>10 mM。为了获得更高的浓度，可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
|
反应条件 |
N/A |
|
应用 |
在临床前和早期临床研究中，ABT-263具有抗肿瘤效应。在体外，ABT-263与Bcl-2、Bcl-xL和Bcl-w结合，在体内仅靶向结合Bcl-2。在人非霍奇金（non-Hodgkin）淋巴瘤中，ABT-263抑制Bcl-2的高表达，从而提高促凋亡蛋白Bim的水平。 |
| 动物实验[2]： | |
|
动物模型 |
免疫缺陷NOD/SCID或NOD/SCID，ILγ受体阴性小鼠 |
|
剂量 |
100 mg/kg/day，21天；口服给药 |
|
应用 |
ABT-263可以很大程度上抑制患者来源的小儿急性淋巴细胞白血病异种移植物的活性。ABT-263的敏感性与MCL1 mRNA的低表达水平相关。BH3分析表明，ABT-263的耐受性与NOXA肽引发的线粒体启动相关。 |
|
注意事项 |
请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的，属于正常现象。 |
|
References: 1. Mérino D1, Khaw SL, Glaser SP et al. Bcl-2, Bcl-x(L), and Bcl-w are not equivalent targets of ABT-737 and navitoclax (ABT-263) in lymphoid and leukemic cells.Blood. 2012 Jun 14;119(24):5807-16. 2. Suryani S, Carol H, Chonghaile TN et al. Cell and Molecular Determinants of In Vivo Efficacy of the BH3 Mimetic ABT-263 against Pediatric Acute Lymphoblastic Leukemia Xenografts. Clin Cancer Res. 2014 Jul 10. |
|
| ABT-263 (Navitoclax)是Bcl-xL、 Bcl-2和Bcl-w的抑制剂，Ki值分别为Ki≤ 0.5 nM、≤1 nM 和≤1 nM。. | ||||||
| 靶点 | Bcl-xL | Bcl-2 | Bcl-w | |||
| IC50 | ≤ 0.5 nM (Ki) | ≤1 nM (Ki) | ≤ 1 nM (Ki) | |||
质量控制和MSDS
- 批次:
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