| 规格 | 价格 | 库存 | 数量 |
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| 10 mM * 1 mL in DMSO |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
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| 体外研究 (In Vitro) |
Tanespimycin 可降解依赖于视网膜母细胞瘤以及突变型和野生型 AR 的前列腺癌细胞的 HER2、Akt 和 G1 生长停止。 tantespimycin 的 IC50 值范围为 25 至 45 nM（LNCaP，25 nM；LAPC-4，40 nM；DU-145，45 nM；PC-3，25 nM），可抑制前列腺癌细胞系 [1]。 Tanespimycin (0.1–1 μM) 会导致过度表达 ErbB2 的乳腺癌细胞几乎完全失去 ErbB2[2]。 Tanespimycin 下调 Bcl-2、Survivin 和 Cyclin B1，并上调裂解的 PARP。这些作用阻止 CCA 细胞的发育并导致 G2/M 细胞周期停滞和凋亡[3]。
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| 体内研究 (In Vivo) |
在前列腺癌异种移植物中，tantespimycin（25-200 mg/kg，腹腔注射）以剂量依赖性方式降低 AR、HER2 和 Akt 的表达。当剂量高到足以引起 HER2、Akt 和 AR 降解时，坦替匹霉素剂量依赖性地抑制雄激素依赖性和非依赖性前列腺癌异种移植物的生长，而不引起毒性[1]。通过尾静脉注射，tanespimycin (60 mg/kg) 和 Rapamycin (30 mg/kg) 通过抑制 A549 和 MDA-MB-231 肿瘤的生长来影响 MDA-MB-231 荷瘤大鼠的肿瘤治愈 [4]。
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| 动物实验 |
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| 参考文献 |
[1]. Solit DB, et al. 17-Allylamino-17-demethoxygeldanamycin induces the degradation of androgen receptor and HER-2/neu and inhibits the growth of prostate cancer xenografts.Clin Cancer Res, 2002, 8(5), 986-993.
[2]. Raja, Srikumar M., et al. 17-AAG induces enhanced ubiquitinylation and lysosomal pathway-dependent ErbB2 degradation and cytotoxicity in ErbB2-overexpressing breast cancer cells. Cancer Biology & Therapy (2008), 7(10), 163 [3]. Zhang J, et al. The heat shock protein 90 inhibitor 17-AAG suppresses growth and induces apoptosis in human cholangiocarcinoma cells.Clin Exp Med. 2012 Sep 7. [4]. Newman B, et al. HSP90 Inhibitor 17-AAG Selectively Eradicates Lymphoma Stem Cells.Cancer Res. 2012 Sep 1;72(17):4551-61. Epub 2012 Jun 29. [5]. Kamal A, et al. A high-affinity conformation of Hsp90 confers tumour selectivity on Hsp90 inhibitors. Nature. 2003 Sep 25;425(6956):407-10. [6]. Enomoto A, et al. The HSP90 inhibitor 17-allylamino-17-demethoxygeldanamycin modulates radiosensitivity by downregulating serine/threonine kinase 38 via Sp1 inhibition. Eur J Cancer. 2013 Nov;49(16):3547-58 |
| 分子式 |
C31H43N3O8
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| 分子量 |
585.69
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| CAS号 |
75747-14-7
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| 相关CAS号 |
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| SMILES |
NC(O[C@@H](/C(C)=C/[C@H](C)[C@@H](O)[C@@H](OC)C[C@H](C)CC1=C2NCC=C)[C@@H](OC)/C=C/C=C(C)/C(NC(C1=O)=CC2=O)=O)=O
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| InChi Key |
AYUNIORJHRXIBJ-HTLBVUBBSA-N
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| InChi Code |
InChI=1S/C31H43N3O8/c1-8-12-33-26-21-13-17(2)14-25(41-7)27(36)19(4)15-20(5)29(42-31(32)39)24(40-6)11-9-10-18(3)30(38)34-22(28(21)37)16-23(26)35/h8-11,15-17,19,24-25,27,29,33,36H,1,12-14H2,2-7H3,(H2,32,39)(H,34,38)/b11-9+,18-10+,20-15+/t17-,19+,24+,25+,27-,29+/m1/s1
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| 化学名 |
(4E,6E,8S,9S,10E,12S,13R,14S,16R)-19-(allylamino)-13-hydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl carbamate.
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| 别名 |
NSC330507; CP127374; 17-AAG, BAY 579352, KOS-953, 17 AAG, CP-127374, NSC-330507, NSC 330507; CP 127374; 17AAG, BAY 57-9352, BAY579352, KOS 953, KOS953, Tanespimycin
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| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| 溶解度 (体外) |
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| 溶解度 (体内) |
Solubility in Formulation 1: ≥ 5 mg/mL (8.54 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (8.54 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 5 mg/mL (8.54 mM) in 15% Cremophor EL + 85% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Solubility in Formulation 4: ≥ 1.62 mg/mL (2.77 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.2 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.. Solubility in Formulation 5: 5%DMSO+corn oil: 10 mg/mL 1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL； 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果，工作液请现配现用！ 6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
| 制备储备液 | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7074 mL | 8.5369 mL | 17.0739 mL | |
| 5 mM | 0.3415 mL | 1.7074 mL | 3.4148 mL | |
| 10 mM | 0.1707 mL | 0.8537 mL | 1.7074 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液)：对于大多数产品，InvivoChem推荐用DMSO配置母液 (比如：5、10、20mM或者10、20、50 mg/mL浓度），个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息，或者很难将产品溶解在溶液中，请联系我们;
3、建议使用下列计算器进行相关计算（摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等）;
4、母液配好之后，将其分装到常规用量，并储存在-20°C或-80°C，尽量减少反复冻融循环。
计算结果:
工作液浓度： mg/mL；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度，请首先与我们联系。
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH2O，混匀澄清。
(1) 请确保溶液澄清之后，再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶；
(2) 一定要按顺序加入溶剂 (助溶剂) 。
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00118248 | Completed Has Results | Drug: tanespimycin | Recurrent Thyroid Cancer Stage IV Follicular Thyroid Cancer |
National Cancer Institute (NCI) | December 2004 | Phase 2 |
| NCT00564928 | Completed | Drug: IPI-504 | Prostate Cancer Prostatic Neoplasms |
Infinity Pharmaceuticals, Inc. | November 2007 | Phase 2 |
| NCT00098423 | Completed | Drug: tanespimycin Drug: cytarabine |
Accelerated Phase Chronic Myelogenous Leukemia |
National Cancer Institute (NCI) | November 2004 | Phase 1 |
| NCT00093821 | Completed | Drug: tanespimycin | Childhood Chronic Myelogenous Leukemia |
National Cancer Institute (NCI) | September 2004 | Phase 1 |
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