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ABT-737

现货
Catalog No.
A8193
Bcl-2抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 850.00
现货
5mg
¥ 500.00
现货
10mg
¥ 900.00
现货
50mg
¥ 3,000.00
现货
100mg
¥ 4,800.00
现货
500mg
¥ 13,000.00
现货

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Background

ABT-737 is a novel and potent inhibitor of B-cell lymphoma 2 (BCL-2) family proteins, which are critical for cell survival and overexpressed in many tumor cells, with high affinity towards BCL-XL, BCL-2, and BCL-w but no affinity towards less homologous proteins, such as BCL-B, MCL-1, and A1. ABT-737 has shown single-agent activity against lymphoma and small-cell lung cancer as well as substantial antimyeloma activity both in vitro and in vivo. In recent studies, acute myeloid leukemia blast, origenitor, and stem cells are effectively killed by ABT-737 with normal hematopoietic cells intact. The disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway could also be induced by ABT-737.

Reference

Marina Konopleva, Rooha Contractor, Twee Tsao, Ismael Samudio, Peter P. Ruvolo, Shinichi Kitada, Xingming Deng, Dayong Zhai, Yue-Xi Shi, Thomas Sneed, Monique Verhaegen, Maria Soengas, Vivian R. Ruvolo, Teresa McQueen, Wendy D. Schober, Julie C. Watt, Tilahun Jiffar, Xiaoyang Ling, Frank C. Marini, David Harris, Martin Dietrich, Zeev Estrov, James McCubrey, W. Stratford May, John C. Reed, and Michael Andreeff. Mechanisms of apoptosis sensitivity and resistance to the BH3 mimetic ABT-737 in acute myeloid leukemia. Cancer Cell 2006: 10; 375-388

Suzanne Trudel, A. Keith Stewart, Zhihua Li, Yanjun Shu, Sheng-Ben Liang, Young Trieu, Donna Reece, Josh Paterson, Dingyan Wang, and Xiao-Yan Wen. The Bcl-2 family protein inhibitor,ABT-737, has substantial antimyeloma activity and shows synergistic effect with dexamethasone and melphalan. Clin Cancer Res 2007; 13 (2) 621-629

文献引用

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt813.43
Cas No.852808-04-9
FormulaC42H45ClN6O5S2
SynonymsABT 737, ABT737
Solubility≥40.67mg/mL in DMSO, <2.29 mg/mL in EtOH, <2.55 mg/mL in H2O
Chemical Name4-[4-[[2-(4-chlorophenyl)phenyl]methyl]piperazin-1-yl]-N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonylbenzamide
SDFDownload SDF
Canonical SMILESCN(C)CCC(CSC1=CC=CC=C1)NC2=C(C=C(C=C2)S(=O)(=O)NC(=O)C3=CC=C(C=C3)N4CCN(CC4)CC5=CC=CC=C5C6=CC=C(C=C6)Cl)[N+](=O)[O-]
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。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。

试验操作

细胞实验:

细胞系

小细胞肺癌(SCLC)细胞系(NCI-H889、NCI-H1963、NCI-H1417、NCI-H146、NCI-187、DMS79、NCI-1048、NCI-H82、NCI-H196、H69AR和DMS114)。

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

48 h;10 μM

应用

ABT-737作为单药活性抑制细胞增殖的能力在11种SCLC细胞系中进行评估。在H146细胞中,用活化caspase 3的底物Ac-DEVD-AMC处理24小时,ABT-737剂量依赖地增加细胞凋亡,与其剂量依赖地减少细胞活力一致,表明ABT-737通过诱导细胞凋亡,从而抑制细胞增殖。

动物实验:

动物模型

淋巴瘤多发Eμ-myc转基因小鼠

剂量

75 mg/kg;尾部注射

应用

与对照组小鼠相比,ABT-737(75 mg/kg)治疗小鼠的骨髓和脾脏中所有B淋巴细胞亚群均显著减少。ABT-737治疗的Eμ- myc动物骨髓中具有显著更多的凋亡细胞(**P<0.01)。

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] Tahir S K, Yang X, Anderson M G, et al. Influence of Bcl-2 family members on the cellular response of small-cell lung cancer cell lines to ABT-737[J]. Cancer research, 2007, 67(3): 1176-1183.

[2] Kelly P N, Grabow S, Delbridge A R D, et al. Prophylactic treatment with the BH3 mimetic ABT-737 impedes Myc-driven lymphomagenesis in mice[J]. Cell Death & Differentiation, 2012, 20(1): 57-63.

生物活性

ABT-737是一种BH3模拟抑制剂,作用于Bcl-xL、Bcl-2和Bcl-w,非细胞试验中EC50分别为78.7 nM、30.3 nM和197.8 nM,但对Mcl-1、Bcl-B及Bfl-1没有抑制作用。
靶点 Bcl-xL Bcl-2 Bcl-w      
IC50 78.7 nM (EC50) 30.3 nM (EC50) 197.8 nM (EC50)      

质量控制

化学结构

ABT-737

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