Tanespimycin (17-AAG)

製品コードS1141 バッチS114106

印刷

化学情報

Synonyms

CP127374, NSC-330507, KOS 953

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₃₁H₄₃N₃O₈

分子量

585.69

CAS No.

75747-14-7

Solubility (25°C)*

体外

DMSO

100 mg/mL (170.73 mM)

Ethanol

10 mg/mL (17.07 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	10.000mg/ml (17.07mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	6.000mg/ml (10.24mM)	Taking the 1 mL working solution as an example, add 50 μL of 120 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) is a potent HSP90 inhibitor with IC50 of 5 nM in a cell-free assay, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. Tanespimycin (17-AAG) induces apoptosis, necrosis, autophagy and mitophagy. Phase 3.
in vitro	Tanespimycin (17-AAG), an analog of geldanamycin, exhibits greater than 100 times higher binding affinity for Hsp90 derived from HER-2-overexpressing cancer cells (BT474, N87, SKOV3 and SKBR3) or BT474 breast carcinoma cells with IC50 values of 5-6 nM. ^[1] It causes the degradation of HER2, HER3, Akt, and both mutant and wild-type androgen receptor (AR), leading to the RB-dependent G1 growth arrest of prostate cancer cells such as LNCaP, LAPC-4, DU-145, and PC-3 with IC50 values of 25-45 nM. ^[2] In addition to inducing apoptosis of Ba/F3 cells transformed with wild-type BCR-ABL with an IC50 of 5.2 μM, this compound has the ability to induce apoptosis of cells transformed with T315I and E255K BCR-ABL mutants with IC50 values of 2.3 μM and 1.0 μM, respectively, by inducing the degradation of both wild-type BCR-ABL protein and mutants. ^[3]
in vivo	Tanespimycin (17-AAG) displays significantly higher binding affinity for Hsp90 from 3T3-src, B16 or CT26 xenografts in nude mice with IC50 values of 8-35 nM as compared with that from the normal tissues with IC50 values of 200-600 nM. ^[1] Administration of this compound (~50 mg/kg) causes significant decline in AR, HER2, HER3, and Akt expression in a dose-dependent manner with >50% decline at dose of 50 mg/kg, resulting in the dose-dependent inhibition of androgen-dependent (CWR22) and -independent (CWR22R and CWRSA6) prostate cancer xenografts growth by 67%, 80% and 68% at dose of 50 mg/kg, respectively. ^[2]
特徴	Displays very low toxicity toward normal cells.

プロトコル(参考用のみ)

キナーゼアッセイ	Hsp90 binding assays
キナーゼアッセイ	Purified native Hsp90 protein or cell lysates from HER-2-overexpressing cancer cells (BT474, N87, SKOV3 and SKBR3) or BT474 breast carcinoma cells in lysis buffer (20 mM HEPES, pH 7.3, 1 mM EDTA, 5 mM MgCl₂, 100 mM KCl) are incubated with various concentrations of Tanespimycin (17-AAG) for 30 minutes at 4 °C, and then incubated with biotin-GM linked to BioMag streptavidin magnetic beads for 1 hour at 4 °C. Tubes are placed on a magnetic rack, and the unbound supernatant removed. The magnetic beads are washed three times in lysis buffer and heated for 5 minutes at 95 °C in SDS–PAGE sample buffer. Samples are analysed on SDS protein gels, and western blots done using indicated antibodies. Bands in the western blots are quantified using the Bio-rad Fluor-S MultiImager, and the percentage inhibition of binding of Hsp90 to the biotin-GM is calculated. The IC50 reported is the concentration of this compound needed to cause half-maximal inhibition of binding.
細胞アッセイ	細胞株	BT474, SKBR3, N87, SKOV3, MCF7, MDA468, Hs578T, Hs578Bst, A549, HT29, U87, SKMG3, HT1080, RPTEC, NDF, HMVEC, HMEC, HUVEC, and PBMC cells
	濃度	Dissolved in DMSO, final concentrations ~10 μM
	反応時間	5 days
	実験の流れ	Tanespimycin (17-AAG) is added at increasing concentrations and incubated for 5 days after cells are seeded in 96-well plates at 2,000 cells per well in a final culture volume of 100 μL for 24 hours. Viable cell number is 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 is subtracted. Percentage of viable cells = (A₄₉₀ of this compound treated sample/A₄₉₀ untreated cells) × 100. The IC50 is defined as the concentration that gave rise to 50% viable cell number.
動物実験	動物モデル	Male nu/nu athymic mice inoculated s.c. with androgen-dependent CWR22 xenograft, and female nu/nu athymic mice inoculated s.c. with androgen-independent xenografts CWR22R and CWRSA6
	投薬量	~50 mg/kg
	投与方法	Injection i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/14508491/
https://pubmed.ncbi.nlm.nih.gov/12006510/
https://pubmed.ncbi.nlm.nih.gov/12351420/

カスタマーフィードバック

: Data from [Data independently produced by Mol Cancer, 2014, 13, 150]

: Data from [Data independently produced by Oncotarget, 2014, 5, 4269-82]

: Data from [Mol Cell Biol, 2013, 33(12), 2375-87]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

A patient-derived T cell lymphoma biorepository uncovers pathogenetic mechanisms and host-related therapeutic vulnerabilities [ Cell Rep Med, 2025, S2666-3791(25)00102-8]	PubMed: 40147445
TBK1 is a signaling hub in coordinating stress-adaptive mechanisms in head and neck cancer progression [ Autophagy, 2025, 1-23.]	PubMed: 40114316
NASP implication in the androgen receptor associated with castration resistance in prostate cancer [ Cell Commun Signal, 2025, 23(1):331]	PubMed: 40640803
HSP90 deficiency promotes cholesteryl ester accumulation in lipid droplets via endocytosis of low-density lipoprotein [ Commun Biol, 2025, 8(1):1169]	PubMed: 40770403
Heat shock protein 90 chaperone activity is required for hepatitis A virus replication [ J Virol, 2025, e0050225]	PubMed: 40470959
Targeting HSP90 with Ganetespib to Induce CDK1 Degradation and Promote Cell Death in Hepatoblastoma [ Cancers (Basel), 2025, 17(8)1341]	PubMed: 40282517
Topical application of the HSP90 inhibitor 17-AAG reduces skin inflammation and partially restores microbial balance: implications for atopic dermatitis therapy [ Sci Rep, 2025, 15(1):21245]	PubMed: 40593012
Role of the NuRD complex and altered proteostasis in cancer cell quiescence [ bioRxiv, 2025, 2025.02.10.637435]	PubMed: 39990343
Pan-cancer proteogenomics expands the landscape of therapeutic targets [ Cell, 2024, S0092-8674(24)00583-X]	PubMed: 38917788
Pan-cancer proteogenomics expands the landscape of therapeutic targets [ Cell, 2024, S0092-8674(24)00583-X]	PubMed: 38917788

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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