| Size | Price | Stock | Qty |
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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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Purity: ≥98%
Tanespimycin (formerly NSC-330507; CP-127374; 17-AAG, BAY-579352, KOS-953, 17-AAG, CP-127374), a benzoquinone analog and a derivative of the antibiotic geldanamycin, is an orally bioavailable and small-molecule inhibitor of heat shock protein 90/HSP90 with potential antitumor activity. It inhibits HSP90 with an IC50 of 5 nM in a cell-free assay. Tanespimycin is being studied for the treatment of cancer, specifically in younger patients with certain types of leukemia or solid tumors, especially kidney tumors.
| ln Vitro |
Tanespimycin degrades HER2, Akt, and the G1 growth halt of prostate cancer cells that is dependent on retinoblastoma as well as mutant and wild-type AR. With IC50 values ranging from 25 to 45 nM (LNCaP, 25 nM; LAPC-4, 40 nM; DU-145, 45 nM; and PC-3, 25 nM), tantespimycin suppresses prostate cancer cell lines [1]. Tanespimycin (0.1–1 μM) causes breast cancer cells that overexpress ErbB2 to almost completely lose ErbB2[2]. Tanespimycin downregulates Bcl-2, Survivin, and Cyclin B1, and upregulates cleaved PARP. These effects prevent the development of CCA cells and cause G2/M cell cycle arrest and apoptosis[3].
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| ln Vivo |
In prostate cancer xenografts, tantespimycin (25–200 mg/kg, ip) reduces AR, HER2, and Akt expression in a dose-dependent manner. At doses high enough to cause the degradation of HER2, Akt, and AR, tantespimycin dose-dependently suppresses the growth of androgen-dependent and -independent prostate cancer xenografts without causing toxicity [1]. Through tail vein injection, tanespimycin (60 mg/kg) and Rapamycin (30 mg/kg) impacted tumor cure in MDA-MB-231 tumor-bearing rats by inhibiting the growth of A549 and MDA-MB-231 tumors [4].
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| Animal Protocol |
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| References |
[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 |
| Molecular Formula |
C31H43N3O8
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| Molecular Weight |
585.69
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| CAS # |
75747-14-7
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| Related CAS # |
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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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| Chemical Name |
(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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| Synonyms |
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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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
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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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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