ABT-737
目录号：S1002
Molecular Weight(MW): 813.43
ABT-737是一种BH3模拟抑制剂，作用于Bcl-xL，Bcl-2和Bcl-w，无细胞试验中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。Phase 2。
客户使用该产品的17个实验数据：
-
Cardiomyocytes transduced with or without Ad-Mst1 were treated with ABT-737 (0, 0.1, 1, 10 uM) for 12 hours. Representative immunoblots with antibodies to p62/SQSTM1, LC3 and GAPDH are shown.
Nat Med 2013 19(11), 1478-88. ABT-737 purchased from Selleck.
Release of mitochondrial cytochrome c and loss of mitochondrial membrane potential after exposure to ABT-737 (100nM) for 2 hours were assessed by immunohistochemistry and staining with TMRE (red, top panels) and anti-CD41/FITC (green, top panels). Bar represents 5 um. Note that control cells display spreading on glass slides, whereas ABT-737-treated cells do not.
Blood 2011 17(26), 7145-54. ABT-737 purchased from Selleck.
-
Platelets were incubated in HBS with or without ABT-737 (100nM) for 2 hours before analysis by immunohistochemistry and confocal microscopy. Actin was stained using phalloidin/Alexa-488 (green), and tubulin was stained using anti-tubulin/phycoerythrin (red). Bar represents 5 uM.
Blood 2011 17(26), 7145-54. ABT-737 purchased from Selleck.
BCL-XL mediates human neutrophil survival. PMNs were preincubated with the BH3 mimetic ABT-737 (1–10 μM), then cultured in normoxia (gray bars) with or without GM-CSF (500 U/ml) or hypoxia (white bars)or 20 hours, and apoptosis was assessed by morphology (n = 4).
J Clin Invest 2011 121, 1053-1063. ABT-737 purchased from Selleck.
-
Analysis of SW480 and SW620 cell sensitivity to the BH3-mimetic ABT-737. (a, b) Percentage of apoptosis in adherent or suspended SW480 (a) or SW620 (b) cells cultured in the presence (ABT-737) or absence (ctrl) of ABT-737 (1 uM).
Cell Death Dis 2013 4, e801. ABT-737 purchased from Selleck.
(B) The sensitivity (LD50) of CLL cells, assessed by annexin V staining after 48 h of treatment with ABT‐737, ABT‐263 or ABT‐199, was plotted against the pBcl‐2/Bcl‐2, Mcl‐1/Bcl‐2 and (pBcl‐2 + Mcl‐1)/Bcl‐2 ratios. Relative protein quantification was carried out with kodak carestream molecular imaging software and normalized to β‐actin. Spearman's correlation (r) and P values are shown. Data shown are representative of five independent experiments.
Br J Pharmacol, 2016, 173(3):471-83. ABT-737 purchased from Selleck.
-
Bcl-XL/Bcl-2 inhibitor ABT-737 aggravates the proapoptotic effects of IL-1IFN-. INS-1E cells were transfected with single or smart Pool PUMA siRNAs and exposed to ABT-737 for 24 h. At this time point, cell death was measured by HO/PI, n 3. *, p 0.05; **, p 0.01.
J Biol Chem 2010 285, 19919-19920. ABT-737 purchased from Selleck.
Effect of ABT-737 on the cell viability of CCRF-CEM cells by treatments of AY4 (10 μg/ml), TRAIL (0.5 μg/ml), SAHA (1 μM),VPA (1 mM), or ABT-737 (10 μM) alone or in combination for 24 h prior to MTT assay.
Apoptosis 2010 15, 1256-1269. ABT-737 purchased from Selleck.
-
Effects of ABT-737 and RES, applied alone and in combination, on the viability of MOLT-4 cells.
Toxicol In Vitro, 2017, 42:38-46. ABT-737 purchased from Selleck.
Upper panel ABT-737 inhibits TFK-1 and EGI-1 cell growth.Cells were exposed to ABT-737 at a concentration ranging from 1 to 50 lM. Following 72 h of incubation, growth inhibition was analyzed by crystal violet assay. Dose–effect plot of ABT-737 treatment is presented.
Cancer Chemoth Pharm 2011 67, 557-567. ABT-737 purchased from Selleck.
-
Lower panel detection of PARP-1, cleaved caspase-9 and caspase-3, BCL-2 and MCL-1 in TFK-1 and EGI-1 cells after 72 h of ABT-737 treatment (1, 3, 10, 25,50 μM). Cell lysates were analyzed on Western blotting.
Cancer Chemoth Pharm 2011 67, 557-567. ABT-737 purchased from Selleck.
Apoptosis induced by BCL2-inhibitors in P-glycoprotein expressing cells. MDCKII wild type or MDR1 cells were exposed to different concentrations of ABT-737 (C) or ABT-263 (D) for 24 h before apoptosis was assessed by flow cytometry using externalization of phosphatidylserine.
Biochem Biophys Res Commun 2012 408, 344-9. ABT-737 purchased from Selleck.
-
GSIXII synergized with ABT-737 to trigger apoptosis in breast cancer cells . Breast cancer cell lines were incubate d for 48 hours with 10μM GSIXII or DMSO (Ct) in combination or not with ABT-737, 1 μM. Then apoptosis was evaluated with Apo2.7 or Annexin-V staining and flow-cytometry analysis. Represented data are the means of positive cells ± SEM, from three independent experiments.(A) Suboptimal concentrations of GSIXII (5 μM) and 1 μM ABT-737 were used alone or in combination in MFU assay in MCF7 and BT549 cell lines. Results were obtained from three independent experiments and compared with mock-treated condition. (B) The 20 μM SAHM1 was used alone or in combination in MFU assay in MCF7 and BT549 cell lines. Results were obtained from three independent experiments and compared with the mock-treated condition.
Biochem Biophys Res Commun 2013 408, 344-9. ABT-737 purchased from Selleck.
3 μM ABT737 inhibited growth and viability of TF-1 cells and potentiated proapoptotic effects of 1 μM BIO after 72 hours treatment. TF-1 cells treated with both drugs exhibited more apoptotic cells compared to those treated with each single drug. ABT737 abrogated the protection from BIO-induced apoptosis provided by MS5 coculture.
Exp Hematol 2010 38, 908-921. ABT-737 purchased from Selleck.
-
The combined use of ABT-737 and sorafenib changes the apoptotic effect. MC-3 cells were treated with the indicated compounds for 48 h. (A) Nuclear condensation and fragmentation were evaluated in DAPI-stained cells as described in the Materials and Methods (X400). (B) Live (green) and dead (red) cells were qualified using the Live/dead assay kit as described in the Materials and Methods (X200). (For interpretation of the references to colour in this figure legend, the reader is referred to the web version of this article.)
Arch Oral Biol, 2017, 73:1-6. ABT-737 purchased from Selleck.
MEF wt and MEF Mcl-1 ko mice activating active caspase-3 using 1um ABT for 24h
Dr. Arnim Weber of Medizinische Mikrobiologie und Hygiene Universitatsklinikum Freiburg. ABT-737 purchased from Selleck.
-
MDB-MA-231 cells were exposed to 30 um cisplatin in the absence or in thepresence of 100nm ABT-737.The cell were stained with Hoechst 33342,MitoTracker Red and Yo-pro-1.
Dr. Zhang of Tianjin Medical University. ABT-737 purchased from Selleck.
产品安全说明书
Bcl-2抑制剂选择性比较
生物活性
| 产品描述 | ABT-737是一种BH3模拟抑制剂，作用于Bcl-xL，Bcl-2和Bcl-w，无细胞试验中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。Phase 2。 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 特性 | ABT-737是第一代抗凋亡BCL-2家族蛋白小分子抑制剂。 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 靶点 |
|
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 体外研究 |
ABT-737降低BCL-2/BAX异质二聚体,而诱导HL60细胞凋亡,但是对细胞周期分布没有抑制效果。ABT-737也诱导细胞色素C从线粒体中释放，促进BAX构象改变，BAX与凋亡相关。在白血病模型中，ABT-737按30 mg/kg处理，阻断53%白血病负荷，且使鼠寿命明显延长。ABT-737不会导致血细胞数和血清组成发生异常。[1]通过使Mcl-1失活而使抵抗细胞（Hela和MCF-7）对ABT-737敏感。当Mcl-1无效时，ABT-737也导致BAX/BAK-依赖的细胞色素C释放。ABT-737延长携带BCL-2肿瘤的鼠寿命。[2]ABT-737从BCL2’s BH3结合袋取代BIM,使BIM激活BAX,诱导线粒体透化作用,快速致死慢性淋巴细胞性白血病(CLL)细胞。[3] Noxa正向调节增强H196细胞对ABT-737敏感性。ABT-737抑制多种SCLC细胞系，包括NCI-H889, NCI-H1963, NCI-H1417, NCI-H146等的增殖，并诱导细胞凋亡。最近研究显示，ABT-737作用于ATLL细胞，明显诱导HTLV-1感染的T细胞凋亡。ABT-737按100 mg/kg剂量作用于ATLL鼠模型显示出强抗癌活性。[5] |
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Cell Data |
|
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 体内研究 | ABT-737按30 mg/kg剂量作用于白血病模型，抑制白血病负担值达53% , 且明显延长鼠寿命。ABT-737不会引起血细胞数和血浆化学性质发生变话。[1] ABT-737延长移植BCL-2传感肿瘤的鼠寿命。[2] ABT-737按100 mg/kg剂量作用于ATLL鼠模型具有强抗癌活性。[5] |
推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)
| 激酶实验： |
+ 展开
荧光偏振实验: 测定GST-BCL-2蛋白家族与FITC-BIM BH3域结合的亲和力。100 nM GST-BCL-2家族融合蛋白和不同浓度 ABT-737在PBS温育2分钟。然后，加入20 nM FITC-BIM BH3 肽。进行荧光偏振，测定IC50值。 |
|---|---|
| 细胞实验： |
+ 展开
|
| 动物实验： |
+ 展开
|
参考文献
- [1] Konopleva M, et al. Cancer Cell, 2006, 10(5), 375-388.
- [2] van Delft MF,et al. Cancer Cell, 2006, 10(5), 389-399.
- [3] Del Gaizo Moore V, et al. J Clin Invest, 2007, 117(1), 112-121.
- [4] Tahir SK, et al. Cancer Res, 2007, 67(3), 1176-1183.
- [5] Ishitsuka K, et al. Cancer Lett, 2012, 317(2), 218-225.
- [6] Konopleva M, et al. Cancer Res, 2008, 68(9), 3413-3420.
- [7] Wade M, et al. Cell Cycle, 2008, 7(13), 1973-1982.
- [8] Paoluzzi L, et al. Blood, 2008, 112(7), 2906-2916.
- [9] Li R, et al. Mol Pharmacol, 2009, 75(5), 1231-1239.
溶解度 (25°C)
| 体外 | DMSO | 100 mg/mL (122.93 mM) |
|---|---|---|
| Water | Insoluble | |
| Ethanol | Insoluble | |
| 体内 |
从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)： 30% Propylene glycol, 5% Tween 80, 65% D5W |
30mg/mL |
* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。
化学数据
| 分子量 | 813.43 |
|---|---|
| 化学式 | C42H45ClN6O5S2 |
| CAS号 | 852808-04-9 |
| 稳定性 | powder |
| in solvent | |
| 别名 | N/A |
计算器
摩尔浓度计算器
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。
稀释计算器
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )
在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.
分子量计算器
通过输入化合物的化学式来计算其分子量：
注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2
摩尔浓度计算器
技术支持
在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。
如果有其他问题，请给我们留言。
常见问题及建议解决方法
-
问题 1：
What’s the recommended method about reconstitution of the compound for in vivo animal study?
-
回答：
For oral administration, we suggest the vehicle: 30% Propylene glycol, 5% Tween 80, 65% D5W, at up to 30mg/ml; For injection, ABT-737 can be dissolved in 2% DMSO/50% PEG 300/5% Tween 80/ddH2O at 2.5 mg/ml.
