坦螺旋霉素|T6290

Tanespimycin
75747-14-7

￥514.00 1瓶起订

￥558.00 10瓶起订

￥359.00 5瓶起订

￥919.00 25瓶起订

￥1450.00 50瓶起订

上海更新日期：2024-09-14

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产品详情:

中文名称：: 坦螺旋霉素

英文名称：: Tanespimycin

CAS号：: 75747-14-7

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.83%

产品类别：: 抑制剂

货号：: T6290

Product Introduction

Bioactivity

名称	Tanespimycin
描述	Tanespimycin (KOS 953) (17-AAG) is an inhibitor of Hsp90 that selectively inhibits BT474 tumor cell Hsp90 (IC50: 5 nM).
细胞实验	Cells were seeded in 96-well plates at 2,000 cells per well in a final culture volume of 100 μl for 24 h before the addition of increasing concentrations of 17-AAG that was incubated for 5 days. Viable cell number was determined using the Celltiter 96 AQueous Nonradioactive Cell Proliferation Assay. The value of the background absorbance at 490 nm (A490) of wells not containing cells was subtracted. Percentage of viable cells ? (A490 of 17-AAG treated sample/A490 untreated cells) × 100. The IC50 was defined as the concentration that gave rise to 50% viable cell number [1].
激酶实验	Purified native Hsp90 protein or cell lysates in lysis buffer (20 mM HEPES, pH 7.3, 1 mM EDTA, 5 mM MgCl2, 100 mM KCl) were incubated with or without 17-AAG for 30 min at 4 °C, and then incubated with biotin-GM linked to streptavidin magnetic beads for 1 h at 4 °C. Tubes were placed on a magnetic rack, and the unbound supernatant removed. The magnetic beads were washed three times in lysis buffer and heated for 5 min at 95 °C in SDS–PAGE sample buffer. Samples were analyzed on SDS protein gels, and western blots done using indicated antibodies. Bands in the western blots were quantified, and the percentage inhibition of binding of Hsp90 to the biotin-GM was calculated. The IC50 reported is the concentration of 17-AAG needed to cause half-maximal inhibition of binding. For in vitro reconstitution, 5 μM of purified Hsp90 was combined with 1 μM each of Hsp70, Hsp40, p23, and Hop purified proteins [1].
动物实验	B10.BR mice were inoculated with 5×10^5 lymphoma cells through intraperitoneal injection. Seven days following tumor implantation, the mice were I.P. injected with 17-AAG or vehicle (10% DMSO + 40% Cremophor EL: Ethanol (3:1) (v/v) + 50 % PBS) every other day for three weeks. At the cessation of treatment, mice were monitored up to 80 days post tumor cell injection. To determine the effects of 17-AAG on lymphoma initiation in vivo, secondary B10.BR recipient mice were implanted by intraperitoneal injection of 1×10^5 lymphoma cells from the spleens of first-round mice that had been treated with 17-AAG or vehicle. These mice were followed up to 160 days post tumor cell injection to monitor differences in tumor initiation between the mice [4].
体外活性	源自肿瘤细胞的Hsp90与Tanespimycin的结合亲和力是正常细胞中Hsp90的100倍。体外重组Hsp90伴侣复合物后，其与Tanespimycin的结合亲和力增强，且ATP酶活性增加[1]。Tanespimycin能促进HER2、Akt以及突变型和野生型AR的降解，并导致依赖视网膜母细胞瘤的G1期生长阻滞在前列腺癌细胞中[2]。Tanespimycin与Trastuzumab联合处理ErbB2过表达的乳腺癌细胞系，增强了ErbB2的泛素化、从细胞表面的下调及溶酶体降解[3]。
体内活性	在非毒性剂量下，Tanespimycin导致前列腺癌异种移植瘤中AR、HER2和Akt表达水平呈剂量依赖性下降。这种下降速度很快，HER2和AR表达在4小时内分别下降了97%和80% [2]。相比之下，接受了Tanespimycin（5至40 mg/kg）治疗的小鼠的脾脏明显变小，脾脏中渗透的淋巴瘤细胞减少，转移至其他器官的癌细胞也显著降低，与接受车辆对照组治疗的小鼠相比。此外，接受Tanespimycin治疗的小鼠比仅接受车辆处理的小鼠存活时间显著延长 [4]。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 22.5 mg/mL (38.42 mM), Sonication is recommended.
关键字	tumor \| stk38 \| Inhibitor \| KOS953 \| cancer \| prostate \| HSP \| Heat shock proteins \| Mitophagy \| NSC-330507 \| Mitochondrial Autophagy \| Tanespimycin \| Apoptosis \| CP127374 \| inhibit \| Autophagy \| CP-127374 \| HER2 \| KOS-953 \| A549 \| NSC330507 \| Bacterial \| Antibiotic
相关产品	Guanidine hydrochloride \| Doxycycline \| Neomycin sulfate \| Hydroxychloroquine \| Dimethyl sulfoxide \| Sulfamethoxazole sodium \| Paeonol
相关库	抑制剂库 \| 微生物天然产物库 \| 经典已知活性库 \| 已知活性化合物库 \| 激酶抑制剂库 \| 抗衰老化合物库 \| 高选择性抑制剂库 \| 药物功能重定位化合物库 \| 抗癌临床化合物库 \| 抗癌药物库

17-AAG|||CP 127374|||NSC 330507|||KOS 953|||坦螺旋霉素

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