ABT-737 (Synonyms: ABT 737, ABT737) |
| رقم الكتالوجGC17234 |
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, with an IC50 value <1nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 852808-04-9
Sample solution is provided at 25 µL, 10mM.
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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]. ABT 737 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 ABT 737 mediated apoptosis in human renal carcinoma cells. Biochem Biophys Res Commun 502: 187 193, 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. ABT 737 increases cisplatin sensitivity through the ROS ASK1 JNK MAPK signaling axis in human ovarian cancer cisplatin resistant 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 ABT 737 and synergistic antitumor activities in combination with histone deacetylase inhibitors. Blood 113: 1982 1991, 2009.
[5] Cheng R, Liu X, Wang Z,et al. a Bcl 2 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.
| 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 | ABT 737 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: | |
| Cas No. | 852808-04-9 | SDF | |
| المرادفات | ABT 737, ABT737 | ||
| Chemical Name | 4-[4-[[2-(4-chlorophenyl)phenyl]methyl]piperazin-1-yl]-N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonylbenzamide | ||
| Canonical 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-] | ||
| Formula | C42H45ClN6O5S2 | M.Wt | 813.43 |
| الذوبان | ≥ 40.67mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.2294 mL | 6.1468 mL | 12.2936 mL |
| 5 mM | 245.9 μL | 1.2294 mL | 2.4587 mL |
| 10 mM | 122.9 μL | 614.7 μL | 1.2294 mL |
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Quality Control & SDS
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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