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ABT-737 Sale

(Synonyms: ABT 737, ABT737) 目录号 : GC17234

An inhibitor of anti-apoptotic Bcl-2 proteins

ABT-737 Chemical Structure

Cas No.:852808-04-9

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥564.00
现货
5mg
¥525.00
现货
10mg
¥630.00
现货
50mg
¥2,100.00
现货
100mg
¥3,710.00
现货
200mg
¥6,160.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

实验参考方法

Cell experiment:

Cell lines

Small-cell lung cancer (SCLC) cell (NCI-H889, NCI-H1963, NCI-H1417, NCI-H146, NCI-187, DMS79, NCI-1048, NCI-H82, NCI-H196, H69AR, and DMS114) lines.

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

48 h; 10 μM

Applications

The ability of ABT-737 to inhibit cell proliferation with single-agent activity was evaluated against a panel of 11 kinds of SCLC cell lines. Ac-DEVD-AMC, a substrate for activated caspase 3, was used to treatment of H146 cells for 24 h. A dose-dependent increase in apoptosis coincided with a dose-dependent decrease in cell viability following ABT-737 treatment suggesting that ABT-737 inhibits cell proliferation through the induction of apoptosis.

Animal experiment:

Animal models

Lymphoma-prone Eμ- myc transgenic mice

Dosage form

75 mg/kg body weight; the tail injection.

Applications

All B-lymphoid subsets in the ABT-737-treatment (75 mg/kg) cohort were significantly decreased, compared with the vehicle-treated animals, in both the bone marrow and the spleen. Eμ- myc animals treated with ABT-737 contained significantly (**P

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

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.

产品描述

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

[1].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
[2].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

Chemical Properties

Cas No. 852808-04-9 SDF
别名 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
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-]
分子式 C42H45ClN6O5S2 分子量 813.43
溶解度 ≥ 40.67mg/mL in DMSO 储存条件 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℃,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。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 1.2294 mL 6.1468 mL 12.2936 mL
5 mM 0.2459 mL 1.2294 mL 2.4587 mL
10 mM 0.1229 mL 0.6147 mL 1.2294 mL
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