GlpBio

ABT-737

目录号: GC17234纯度: >98.00%同义词: ABT 737, ABT737
ABT-737作为一种BH3模拟药物，是Bcl-2家族的抑制剂，可抑制Bcl2、Bcl-xL和Bcl-w的活性，IC50值<1nM。
ABT-737
Cas No.: 852808-04-9
规格价格库存数量操作
5mg¥525.00现货
1
10mg¥630.00现货
1
50mg¥2,100.00现货
1
100mg¥3,710.00现货
1
200mg¥6,160.00现货
1
10mM (in 1mL DMSO)¥564.00现货
1
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产品描述 Description

ABT-737, as a BH3 analog, is an inhibitor of the Bcl-2 family that suppresses the activity of Bcl-2, Bcl-xL, and Bcl-w[1], with an IC50 value <1nM[2].Bcl-2 and Bcl-xL are two key anti-apoptotic proteins within the Bcl-2 family. They localize to mitochondria and regulate mitochondrial outer membrane permeability. These proteins inhibit apoptosis, and their overexpression is closely associated with the onset and progression of various diseases[3]. ABT737 competitively binds to the BH3 domain, specifically inhibiting the interaction between Bcl-2/Bcl-xL and Bak/Bax, thereby inducing apoptosis through the mitochondrial pathway[4].

In vitro, treatment of cisplatin-resistant ovarian cancer cells A2780/DDP with ABT-737 (0-80μM) for 24-48 hours resulted in a time- and dose-dependent decrease in cell survival rate, while significantly enhancing cisplatin-induced activation levels of JNK and ASK1[4]. Treatment of human UC cells (UMUC3 and 5637) with ABT-737 (0–40μM) for 12 hours significantly inhibited cell survival in a dose-dependent manner[5]. Co-treatment of DLD1 cells with an immunotoxin targeting human transferrin receptor (1ng/mL) and ABT-737 (10μM) for 48 hours resulted in caspase-3 activation, indicating cell death via the apoptotic pathway [6].

In vivo, intra-tracheal administration of 50μL carrier solution containing 100μg ABT-737 significantly alleviated AHR symptoms in mice with airway inflammation models and promoted eosinophil apoptosis[7].In vivo, treatment with ABT-737 (100mg/kg) via intraperitoneal injection for 21 days in patient-derived xenograft (PDX) mouse models of small cell lung cancer (SCLC) resulted in minor tumor shrinkage during the treatment period. Combination therapy with ABT-737 and rapamycin (20mg/kg) produced sustained antitumor activity, leading to tumor regression, with efficacy persisting beyond the treatment period [8].

References:
[1] Ou YC, Li JR, Wang JD, et al. Liao SL, Lu HC and Chen CJ: Aspirin restores ABT737mediated apoptosis in human renal carcinoma cells. Biochem Biophys Res Commun 502: 187193, 2018.
[2] Oltersdorf, T., et al. (2005). An inhibitor of Bcl-2 family proteins induces regression of solid tumours. Nature, 435(7042), 677-681.
[3] Li X, Guo Y, Xing Z, et al. ABT737 increases cisplatin sensitivity through the ROSASK1JNK MAPK signaling axis in human ovarian cancer cisplatinresistant A2780/DDP cells[J]. Oncol Rep. 2024 Sep;52(3):122.
[4] Whitecross KF, Alsop AE, Cluse LA, et al.Lindemann RK and Johnstone RW: Defining the target specificity of ABT737 and synergistic antitumor activities in combination with histone deacetylase inhibitors. Blood 113: 19821991, 2009.
[5] Cheng R, Liu X, Wang Z,et al. a Bcl2 family inhibitor, has a synergistic effect with apoptosis by inducing urothelial carcinoma cell necroptosis. Mol Med Rep. 2021 Jun;23(6):412.
[6] Fitzgerald DJ, Moskatel E, Ben-Josef G,et al.Enhancing immunotoxin cell-killing activity via combination therapy with ABT-737. Leuk Lymphoma. 2011 Jun;52 Suppl 2(Suppl 2):79-81. doi: 10.3109/10428194.2011.569961.
[7] Tian BP, Xia LX, Bao ZQ, et al. Bcl-2 inhibitors reduce steroid-insensitive airway inflammation. J Allergy Clin Immunol. 2017 Aug;140(2):418-430. doi: 10.1016/j.jaci.2016.11.027. Epub 2016 Dec 31. Erratum in: J Allergy Clin Immunol. 2021 Jul;148(1):281.
[8] Gardner EE, Connis N, Poirier JT,et al.Rapamycin rescues ABT-737 efficacy in small cell lung cancer. Cancer Res. 2014 May 15;74(10):2846-56. doi: 10.1158/0008-5472.CAN-13-3460. Epub 2014 Mar 10.

ABT-737作为一种BH3模拟药物，是Bcl-2家族的抑制剂，可抑制Bcl2、Bcl-xL和Bcl-w的活性[1]，IC50值<1nM[2]。Bcl-2和Bcl-xL是Bcl-2家族中两个关键的抗凋亡蛋白，它们定位于线粒体并调控线粒体外膜通透性。这两种蛋白能够抑制细胞凋亡的发生，其高表达与多种疾病的发生发展密切相关[3]。ABT737可通过竞争性结合BH3结构域，特异性抑制Bcl2/BclxL与Bak/Bax的结合，进而通过线粒体凋亡途径诱导细胞凋亡[4]。

在体外，ABT-737（0-80μM）处理顺铂耐药卵巢癌细胞A2780/DDP 24-48h，细胞存活率呈时间和剂量依赖性下降，并且能显著增强顺铂诱导的JNK和ASK1活化水平[4]。ABT-737（0-40μM）处理UC细胞（UMUC3和5637） 12h，以剂量依赖性方式显著抑制了细胞存活率[5]。靶向人转铁蛋白受体的免疫毒素（1ng/mL）与ABT-737（10μM）联合使用处理DLD1细胞48小时时，可观察到caspase 3的激活，表明通过凋亡途径引发了细胞死亡[6]。

在体内，经气管内给药途径给予50μL含100μg ABT-737的载体溶液可显著减轻气道炎症模型小鼠的AHR症状，促进嗜酸性粒细胞凋亡[7]。在体内，ABT-737（100mg/kg）通过腹腔注射治疗SCLC PDX模型小鼠21天，持续治疗期间肿瘤出现微小缩小，ABT-737和雷帕霉素（20mg/kg）联合治疗可产生持续抗肿瘤活性，导致肿瘤消退，并且疗效在治疗期结束后仍持续存在[8]。

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

UC cells

Preparation Method

UC cells were seeded in 96-well plates at 10,000 cells per well and incubated for 24h at 37˚C in 5%CO2. They were treated with ABT-737 at 0, 2.5, 5, 10, 20 and 40µM for 12h.MTT (20µl) was added to each well and incubated for 4h at 37˚C in 5% CO2 . Then, 150µl DMSO was added to each well to dissolve the formazan crystals. Finally, the absorbance was measured at 570nm using an automated microplate reader.

Reaction Conditions

0, 2.5, 5, 10, 20, 40μM; 12h

Applications

ABT737 significantly inhibits UC cell proliferation in a concentration-dependent manner.

Animal experiment [2]:

Animal models

SCLC PDX Model Mice

Preparation Method

UC cells were subcutaneously injected into female C.B.-17 severe combined immunodeficiency (scid) mice aged 4 to 6 weeks at the time of PDX injection/transplantation. When tumor volume reached 150mm³, mice were randomly assigned to treatment groups (5–6 mice per group) and received daily intraperitoneal injections of solvent, ABT-737 (100mg/kg), rapamycin (20mg/kg), etoposide (12mg/kg on days 1, 4, and 9), or combination therapy for 21 days. Tumor volume was measured every 3 days.

Dosage form

100mg/kg/day for 21days; i.p.

Applications

When used alone, ABT-737 induced minimal tumor shrinkage during continuous treatment. Combination therapy with ABT-737 and rapamycin produced sustained antitumor activity, leading to tumor regression in SCLC PDX model mice. The therapeutic effect persisted even after the treatment period concluded.

References:
[1]Cheng R, Liu X, Wang Z, Tang K. ABT737, a Bcl2 family inhibitor, has a synergistic effect with apoptosis by inducing urothelial carcinoma cell necroptosis. Mol Med Rep. 2021 Jun;23(6):412.
[2]Gardner EE, Connis N, Poirier JT, Cope L, Dobromilskaya I, Gallia GL, Rudin CM, Hann CL. Rapamycin rescues ABT-737 efficacy in small cell lung cancer. Cancer Res. 2014 May 15;74(10):2846-56. doi: 10.1158/0008-5472.CAN-13-3460. Epub 2014 Mar 10.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号
852808-04-9
同义词
ABT 737, ABT737
化学名
4-[4-[[2-(4-chlorophenyl)phenyl]methyl]piperazin-1-yl]-N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonylbenzamide
SMILES
CN(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-]
分子式
C42H45ClN6O5S2
分子量
813.43 g/mol
溶解性
≥ 40.67mg/mL in DMSO
保存条件
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°C，然后在超声波浴中震荡一段时间。
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。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol