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TW-37

现货
Catalog No.
A4234
Bcl-2抑制剂,抑制Bcl-2、Bcl-XL和Mcl-1。
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,100.00
现货
10mg
¥ 1,150.00
现货
25mg
¥ 2,600.00
现货
50mg
¥ 4,700.00
现货
100mg
¥ 5,900.00
现货

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Background

TW-37 is a potent small-molecule inhibitor of BCL-2 (Ki = 290 nmol/L), which attenuates BCL-2 activation and inhibits multiple BCL-2 family members including BCL-XL (Ki = 1,110 nmol/L) and MCL-1 (Ki = 260 nmol/L). It binds to the BCL-2 homology domain 3 (BH3) groove of BCL-2 preventing the heterodimerization of proapoptotic proteins (such as Bid, Bim, and Bad) with BCL-2 and subsequently allowing them to induce apoptosis. Recent studies indicate TW-37 is able to inhibit the growth of a broad range of cancer cells (such as breast, prostate, lymphoma, and pancreatic cancer), since it induces S-phase cell cycle arrest with regulation of several important cell cycle related genes, including p27, p57, E2F-1, cdc25A, CDK4, cyclin A, cyclin D1 and cyclin E.

Reference

Zhiwei Wang, Asfar Sohail Azmi, Aamir Ahmad, Sanjeev Banerjee, Shaomeng Wang, Fazlul H. Sarkar, and Ramzi M. Mohammad. TW-37, a small-molecule inhibitor of BCL-2, inhibits cell growth and induces apoptosis in pancreatic cancer: involvement of Notch-1 signaling pathway. Cancer Res 2009;69:2757-2765

Naoki Ashimori, Benjamin D. Zeitlin, Zhaocheng Zhang, Kristy Warner, IIan M. Turkienicz, Aaron C. Spalding, Theodoros N. Teknos, Shaomeng Wang, and Jacques E. Nor. TW-37, a small-molecule inhibitor of BCL-2, mediates S-phase cell cycle arrest and suppresses head and neck tumor angiogenesis. Mol Cancer Ther 2009;8:893-903

文献引用

1.Yang IH, Ahn CH, et al. "Heme Oxygenase-1 is a Key Molecule Underlying Differential Response of TW-37-Induced Apoptosis in Human Mucoepidermoid Carcinoma Cells." Molecules. 2019 May 1;24(9). pii: E1700. PMID:31052354
2.Russo M, Milito A, et al. "CK2 and PI3K are direct molecular targets of quercetin in chronic lymphocytic leukaemia." Oncotarget. 2017 Jun 27;8(26):42571-42587. PMID:28489572

Chemical Properties

StorageStore at -20°C
M.Wt573.7
Cas No.877877-35-5
FormulaC33H35NO6S
SynonymsTW37,TW 37
Solubility≥19.75 mg/mL in DMSO, ≥3.41 mg/mL in EtOH with ultrasonic and warming, <2.28 mg/mL in H2O
Chemical NameN-[4-(2-tert-butylphenyl)sulfonylphenyl]-2,3,4-trihydroxy-5-[(2-propan-2-ylphenyl)methyl]benzamide
SDFDownload SDF
Canonical SMILESCC(C)C1=CC=CC=C1CC2=C(C(=C(C(=C2)C(=O)NC3=CC=C(C=C3)S(=O)(=O)C4=CC=CC=C4C(C)(C)C)O)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: [1]

细胞系

BxPC-3和Colo-357细胞

制备方法

该化合物在DMSO中的溶解度大于10 mM,若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应条件

细胞生长抑制:750 nM,72小时;凋亡诱导:500 nM,48小时(通过膜联蛋白V测量)

实验结果

通过克隆形成实验评估细胞活力。与对照相比,TW-37显著抑制BxPC-3和Colo-357细胞的集落形成。此外,TW-37以剂量和时间依赖性方式诱导凋亡。在Annexin V测定中,凋亡细胞的百分比从对照组的5%-6%增加至BxPC-3和Colo-357细胞系中的12%-14%

动物实验: [1]

动物模型

携带Colo-357异种移植物的雌性ICR-SCID小鼠

给药剂量

静脉注射,20 mg/kg/d

实验结果

TW-37显著抑制体内胰腺肿瘤生长。Western印迹分析显示,TW-37处理小鼠的肿瘤中,Notch-1的表达水平显著低于对照组小鼠。此外,在TW-37处理的肿瘤中,Jagged-1和Notch-1下游靶基因Hes-1的表达下调。

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1] Wang Z, Azmi A S, Ahmad A, et al. TW-37, a small-molecule inhibitor of Bcl-2, inhibits cell growth and induces apoptosis in pancreatic cancer: involvement of Notch-1 signaling pathway. Cancer research, 2009, 69(7): 2757-2765.

生物活性

TW-37是一种新型的非肽类抑制剂,作用于重组的Bcl-2、Bcl-xL和Mcl-1,Ki值分别为0.29 μM、1.11 μM和0.26 μM。.
靶点 Bcl-2 Bcl-xL Mcl-1      
IC50 0.29 μM (Ki) 1.11 μM (Ki) 0.26 μM (Ki)      

质量控制

化学结构

TW-37

相关生物数据

TW-37
As an inhibitor of Bcl-2, TW-37 is effective to reduce cell viability in HG3-CLL cells. Incubating the cells with TW-37 in 96 well plates (3×104 cells per well) for 24h shows a dose-dependent inhibition of cell viability with EC50 value of 1.17μM.[Source: Istituto di Scienze dell’Alimentazione]

相关生物数据

TW-37

相关生物数据

TW-37

相关生物数据

TW-37