Tanespimycin (Synonyms: 坦螺旋霉素; 17-AAG; NSC 330507; CP 127374) 纯度: 99.07%
Tanespimycin (17-AAG) 是有效的 HSP90 抑制剂,IC50 为 5 nM,对肿瘤细胞 HSP90 的亲和性比正常细胞高 100 倍。Tanespimycin 消耗细胞内 STK38/NDR1,并降低 STK38 激酶活性。Tanespimycin 还下调 stk38 基因表达。
Tanespimycin Chemical Structure
CAS No. : 75747-14-7
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Free Sample (0.1-0.5 mg) | Apply now | ||
10 mM * 1 mL in DMSO | ¥770 | In-stock | |
10 mg | ¥700 | In-stock | |
25 mg | ¥1100 | In-stock | |
100 mg | ¥2744 | In-stock | |
200 mg | ¥4185 | In-stock | |
500 mg | 询价 | ||
1 g | 询价 |
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生物活性 |
Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC50 of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90[1][5]. Tanespimycin depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin also downregulates the stk38 gene expression[3]. |
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IC50 & Target[5] |
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体外研究 (In Vitro) |
Tanespimycin causes the degradation of HER2, Akt, and both mutant and wild-type AR and the retinoblastoma-dependent G1 growth arrest of prostate cancer cells. Tanespimycin inhibits prostate cancer cell lines with IC50s ranged from 25-45 nM (LNCaP, 25 nM; LAPC-4, 40 nM; DU-145, 45 nM; and PC-3, 25 nM)[1]. Tanespimycin (0.1-1 μM) induces a nearly complete loss of ErbB2 on ErbB2-overexpressing breast cancer cells[2]. Tanespimycin inhibits cell growth and induces G2/M cell cycle arrest and apoptosis in CCA cells together with the down-regulation of Bcl-2, Survivin and Cyclin B1, and the up-regulation of cleaved PARP[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
Tanespimycin (25-200 mg/kg, i.p.) causes a dose-dependent decline in AR, HER2, and Akt expression in prostate cancer xenografts. Tanespimycin treatment at doses sufficient to induce AR, HER2, and Akt degradation results in the dose-dependent inhibition of androgen-dependent and -independent prostate cancer xenograft growth without toxicity[1]. Tanespimycin (60 mg/kg) with Rapamycin (30 mg/kg) inhibits A549 and MDA-MB-231 tumor growth and effects tumor cures in MDA-MB-231 tumor-bearing animals by tail vein injection[4]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
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Clinical Trial |
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分子量 |
585.69 |
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Formula |
C31H43N3O8 |
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CAS 号 |
75747-14-7 |
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中文名称 |
坦螺旋霉素 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
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溶解性数据 |
In Vitro:
DMSO : 50 mg/mL (85.37 mM; Need ultrasonic) 配制储备液
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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。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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Cell Assay [1] |
For the Alamar Blue proliferation assay, 2-4×103 cells are plated in 96-well plates. Later (48 h), cells are treated with Tanespimycin for 96 h or 0.01% DMSO as control. On day 4, Alamar Blue viability assay is performed as described elsewhere. IC50 and IC90s are calculated as the doses of Tanespimycin required to inhibit cell growth by 50 and 90%, respectively. Cell cycle distribution is assayed as described previously with a Becton Dickinson fluorescence-activated cell sorter and analyzed by the Cell Cycle Multicycle system. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
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Animal Administration [1] |
Tanespimycin is dissolved in an EPL vehicle. To aid in the identification of an optimal dose and schedule, nontumor bearing mice are treated by i.p. injection with 25-200 mg/kg of Tanespimycin 5 days/week for 3 weeks or by the EPL vehicle alone. Serum samples are taken from each group, and equal volumes are pooled on days 5, 10, and 15 of treatment for serum chemistry and liver function analysis. At sacrifice, plasma samples are collected for complete blood count. A gross necropsy is performed on all of the mice, and a complete necropsy, including histopathology, is performed on 1 animal/group. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
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