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  • 化合物 ABT-737|T2099|TargetMol

化合物 ABT-737|T2099|TargetMol

ABT-737
852808-04-9
266 1mg 起订
622 5mg 起订
747 10mg 起订
上海 更新日期:2024-12-02

TargetMol中国(陶术生物)

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联系人:邵小姐
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邮箱:marketing@targetmol.com

产品详情:

中文名称:
化合物 ABT-737
英文名称:
ABT-737
CAS号:
852808-04-9
品牌:
TargetMol
产地:
美国
保存条件:
keep away from direct sunlight,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格:
99.73%
产品类别:
抑制剂
货号:
T2099

Product Introduction

Bioactivity

名称ABT-737
描述ABT-737 is a BH3 mimetic and an inhibitor of Bcl-2, Bcl-xL, and Bcl-w (EC50=30.3 nM/78.7 nM/197.8 nM). ABT-737 exhibits antitumor activity and anti-aging activity.
细胞实验Cells were seeded into 96-well plates (5 × 10^3 cells/well) and cultured for 12 h at 37 °C, as described above. Then, the medium was replaced with RPMI 1640 containing various concentrations of ATO (1, 2, 4 and 8 nM), ABT-737 (2.5, 5, 10 and 20 μM) or combinations of ATO and ABT-737, and cells were cultured for a further for 24, 48 or 72 h at 37 °C. Cells cultured in RPMI 1640 containing an equal volume of 0.01 M phosphate-buffered saline (PBS, pH 7.4; vehicle) served as controls. Cell viability was measured using Cell Counting Kit-8, according to the manufacturer's instructions. The cell proliferation rate was calculated according to the formula: experimental optical density (OD) value/control OD value × 100%. Experiments were repeated in triplicate [2].
激酶实验To determine the binding affinity of GST-BCL-2 family proteins to the FITCconjugated BH3 domain of BIM, FPAs were performed as described. Briefly, 100 nM of GST-BCL-2 family fusion proteins were incubated with serial dilutions of ABT-737 in PBS for 2 min. Then, 20 nM of FITC-BIM BH3 peptide was added. Fluorescence polarization was measured using a Detection System after 10 min using the 96-well black plate. IC50s were determined [1].
动物实验Mice were housed under standard conditions and had free access to water and food, under a 12-h light/12-h dark cycle in a room maintained at 18 – 22 °C and 50 – 65% humidity. SGC7901 cells (5 × 10^6) were subcutaneously inoculated into the right flank of BALB/c mice (H-2b). Tumour volume was measured using callipers and estimated according to the formula: π ? 6 × a2 × b, where a was the short axis, and b was the long axis. After 10 days, when the tumours had reached about 0.2 cm in diameter, the mice were randomly assigned to four groups (n = 8 per group), using a randomization schedule generated by the SAS software package. The groups were: control; ABT-737; ATO; ABT737 + ATO. They received, respectively: vehicle (1% DMSO, 99% 0.01 M PBS; pH 7.4); ABT-737 (50 mg/kg); ATO (2.5 mg/kg); ABT737 (50 mg/kg) + ATO (2.5 mg/kg) intraperitoneally (i.p.) every 2 days. Drugs were dissolved in the vehicle solution. To standardize the experiments, each mouse received a similar volume of solution. After 15 days, the mice were euthanized and the solid SGC-7901 tumours were harvested, fixed with 4% paraformaldehyde, frozen in optimal cutting temperature compound and stored at –80 °C [2].
体外活性方法:AML 细胞系 HL-60 用 ABT-737 (10-250 nM) 处理 24-72 h,通过活细胞计数检测细胞生长。 结果:HL-60 细胞对 ABT-737 显示出高敏感性,IC50=50 nM。[1] 方法:甲状腺癌细胞用 ABT-737 (1 µM) 处理 24 h,通过 flow cytometer 检测细胞周期。 结果:在所分析的所有五个细胞系中,subG1 级细胞显著增加,表明 ABT-737 诱导了细胞死亡和 DNA 断裂。ABT-737 处理的乳头状 BHT101 和间变性 SW1736 细胞中处于 subG1 峰的细胞百分比最高 (54.8% 和 39.9%)。[2]
体内活性方法:为检测体内抗肿瘤活性,将 ABT-737 (20-30 mg/kg,30% propylene glycol+5% Tween 80+65% D5W (5% dextrose in water),pH 4−5) 腹腔注射给注射 luc-FD/ΔRaf-1:ER 细胞的 SCID 小鼠,每天一次,持续 21 天。 结果:ABT-737 在 20 和 30 mg/kg 剂量水平下分别将白血病负担抑制了 48% 和 53%,并显著延长了这种侵袭性白血病模型中小鼠的存活期,中位存活期为 28-32.5 天,而对照组为 19.5 天。[1]
存储条件keep away from direct sunlight,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 50 mg/mL (61.47 mM)
关键字Mitophagy | inhibit | mimetic | HCT116 | Apoptosis | BIM | ABT 737 | BH3 | Autophagy | AML | HL-60 | Bcl-2 Family | Mitochondrial Autophagy | BCL-2/BAX | ABT737 | Inhibitor | ABT-737
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ABT-737|TargetMol

公司简介

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起,为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部,化学事业部,生物事业部和新材料部。 从虚拟筛选到实体化合物分子供应;从商业化产品销售到个性化定制合成;从对明确靶点的分子筛选到对明确分子的多靶点筛选,从高通量筛选到化学结构优化,我们都可以满足您的科研用品及技术服务的需求。 经过在中国市场五年的精心耕耘,我们已成为筛选化合物领域优秀的供应商,为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期 (12年)
注册资本 566.2651万人民币
员工人数 100-500人
年营业额 ¥ 1亿以上
经营模式 贸易,试剂,定制,服务
主营行业 化学试剂,生物活性小分子

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