Tanespimycin (Synonyms: 坦螺旋霉素; 17-AAG; NSC 330507; CP 127374)

目錄號: HY-10211 純度: 99.01%: FAQs
Data Sheet SDS COA 產品使用指南

摩爾計算器

Tanespimycin (17-AAG) 是有效的 HSP90 抑制劑，IC₅₀ 為 5 nM，對腫瘤細胞 HSP90 的親和性比正常細胞高 100 倍。Tanespimycin 消耗細胞內 STK38/NDR1，并降低 STK38 激酶活性。Tanespimycin 還下調 stk38 基因表達。

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Tanespimycin Chemical Structure

CAS No. : 75747-14-7

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規(guī)格	價格	是否有貨
10 mM * 1 mL in DMSO	￥770	In-stock
5 mg	￥437	In-stock
10 mg	￥698	In-stock
25 mg	￥1100	In-stock
50 mg	￥1650	In-stock
100 mg	￥2475	In-stock
200 mg		詢價
500 mg		詢價

or 大包裝詢價

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Customer Review

Other Forms of Tanespimycin:

Tanespimycin Hydrochloride 詢價

MCE 顧客使用本產品發(fā)表的 46 篇科研文獻

•Signal Transduct Target Ther. 2024 Jun 28;9(1):159. [Abstract]
•Blood. 2019 Oct 17;134(16):1323-1336. [Abstract]
•Nat Commun. 2023 Jul 26;14(1):4505. [Abstract]
•Nucleic Acids Res. 2020 Aug 20;48(14):7944-7957. [Abstract]
•J Exp Clin Cancer Res. 2018 Mar 27;37(1):70. [Abstract]
•Theranostics. 2018 Feb 15;8(7):2044-2060. [Abstract]

•MedComm (2020). 2024 Nov 9;5(11):e756. [Abstract]
•Cell Commun Signal. 2024 Sep 13.
•Int J Biol Sci. 2023 Feb 27;19(5):1471-1489. [Abstract]
•Cancer Lett. 2023 Apr 6;216154. [Abstract]
•Nano Res. 15 December 2021.
•Cell Death Dis. 2018 Feb 7;9(2):165. [Abstract]
•Phytomedicine. 2024 Nov:134:155937. [Abstract]
•J Transl Med. 2020 Apr 15;18(1):166. [Abstract]
•J Clin Endocrinol Metab. 2024 Sep 17:dgae643. [Abstract]
•Biochem Pharmacol. 2024 Aug 9:116478. [Abstract]
•Am J Cancer Res. 2024 May 15;14(5):2072-2087. [Abstract]
•iScience. 2024 May 15.
•Pharmaceuticals. 2023 Nov 16, 16(11), 1618.
•Molecules. 2023 Nov 17, 28(22), 7639.
•J Proteome Res. 2023 Aug 4. [Abstract]
•Int J Mol Med. 2023 Apr;51(4):32. [Abstract]
•Cell Signal. 2023 Feb 24;110639. [Abstract]
•Cells. 2022 Nov 18;11(22):3671. [Abstract]
•Sci Rep. 2022 Nov 5;12(1):18811. [Abstract]
•Front Microbiol. 2022 Jun 30;13:894356. [Abstract]
•BMJ Open Diabetes Res Care. 2022 Jan;10(1):e002579. [Abstract]
•Commun Biol. 2021 Dec 13;4(1):1391. [Abstract]
•Cell Signal. 2021 Apr 1;110001. [Abstract]
•Viruses. 2021, 13(4), 610.
•Cancers (Basel). 2021 Jan 11;13(2):243. [Abstract]
•Commun Biol. 2020 May 8;3(1):226. [Abstract]
•Front Mol Neurosci. 2018 Nov 6;11:401. [Abstract]
•Mol Cancer Ther. 2016 Sep;15(9):2107-18. [Abstract]
•PLoS One. 2024 Sep 26;19(9):e0310915. [Abstract]
•Biochem Biophys Res Commun. 14 July 2022.
•Prostate. 2022 Jun;82(8):917-932. [Abstract]
•Oncol Lett. March 1, 2022.
•Vet Microbiol. February 2022, 109316.
•Pharm Biol. 2021 Dec;59(1):21-30. [Abstract]
•bioRxiv. 2024 October 06.
•bioRxiv. 2024 Aug 6:2024.03.21.586169. [Abstract]
•Patent. US20220211630A1.
•bioRxiv. January 21, 2022.
•Research Square Preprint. 2021 Jun.
•Patent. US20180263995A1.

IHC

: Tanespimycin purchased from MCE. Usage Cited in: Int J Mol Med. 2023 Apr;51(4):32. [Abstract]; Tanespimycin (17?AAG) inhibits the levels of HSP90 and NLRP3, and decreases GSDMD expression, in MH?S cells.

: Tanespimycin purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Mar 27;37(1):70. [Abstract]; Cells are first treated with commercially available HIF-1α inhibitors, including compounds targeting Top1 (Camptothecin, CPT), Top2 (VP; MX) and HSP90 (17-AAG) as well as 2-ME, and then subjected to Western blotting analysis.

: Tanespimycin purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Feb 7;9(2):165. [Abstract]; Western blot analysis of Hsp70 protein and Hsp90 client proteins IKK and EGFR after 24?h Tan IIA treatment. The Hsp90 inhibitor 17-AAG (10?μM) is included as a positive control

: Tanespimycin purchased from MCE. Usage Cited in: Front Mol Neurosci. 2018 Nov 6;11:401. [Abstract]; Effects of 17-AAG on neurogenesis 4 weeks after SAH.

: Tanespimycin purchased from MCE. Usage Cited in: Mol Cancer Ther. 2016 Sep;15(9):2107-18. [Abstract]; Combination of MDV3100 and 17-AAG leads to decreased AR protein level and transcriptional activity. (A&B) LNCaP (A) and C4-2 (B) cells are treated as indicated for 24 hr, followed by IB against AR, PSA and CHIP. (C&D) 22RV1 (C) and MR49F (D) cells are treated as indicated for 24 hr, followed by IB against AR and HSP90. (E) C4-2 cells are treated as indicated for 24 hr, fractionated into cytoplasm and nuclear, followed by IB against AR and Plk1.

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生物活性
實驗參考方法
純度 & 產品資料
參考文獻

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].

IC₅₀ & Target^[5]

HSP90

5 nM (IC₅₀)

Autophagy

Mitophagy

細胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A-375	IC₅₀	1287 nM Compound: 2, 17-AAG	Antiproliferative activity against human A375 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human A375 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
A-375	IC₅₀	32 nM Compound: 2, 17-AAG	Inhibition of Hsp90 in human A375 cells assessed as pS6 degradation after 24 hrs by high content screening Inhibition of Hsp90 in human A375 cells assessed as pS6 degradation after 24 hrs by high content screening	[PMID: 19552433]
A-375	IC₅₀	4 nM Compound: 2, 17-AAG	Inhibition of Hsp90 in human A375 cells assessed as Hsp70 induction after 24 hrs by high content screening Inhibition of Hsp90 in human A375 cells assessed as Hsp70 induction after 24 hrs by high content screening	[PMID: 19552433]
A-431	IC₅₀	0.069 μM Compound: 17-AAG	Cytotoxicity against human A431 cells after 72 hrs Cytotoxicity against human A431 cells after 72 hrs	[PMID: 22538015]
A-431	IC₅₀	0.07 μM Compound: 17-AAG	Antiproliferative activity against human A431 cells after 72 hrs Antiproliferative activity against human A431 cells after 72 hrs	[PMID: 20655237]
A-431	IC₅₀	89 nM Compound: 17-Aag	Cytotoxicity against human A431 cells after 72 hrs by MTT assay Cytotoxicity against human A431 cells after 72 hrs by MTT assay	[PMID: 25277067]
A549	IC₅₀	> 10 μM Compound: 4; 17-AAG	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay	[PMID: 33189438]
A549	IC₅₀	> 10 μM Compound: 17-AAG	Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay	[PMID: 32663707]
A549	GI₅₀	0.0075 μM Compound: III; 17AAG	Antiproliferative activity against human A549 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay	[PMID: 31655430]
A549	GI₅₀	0.08 μM Compound: 1; 17-AAG	Antiproliferative activity against human A549 cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay Antiproliferative activity against human A549 cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay	[PMID: 33934008]
A549	IC₅₀	0.286 μM Compound: 2; 17-AAG	Antiproliferative activity against human A549 cells after 48 hrs by MTT assay Antiproliferative activity against human A549 cells after 48 hrs by MTT assay	[PMID: 28073608]
A549	IC₅₀	81 nM Compound: 17-Aag	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 25277067]
AU565	IC₅₀	0.003 μM Compound: 2, 17-AAG	Inhibition of Hsp90 in human AU565 cells assessed as Her2 degradation after 24 hrs by high content screening Inhibition of Hsp90 in human AU565 cells assessed as Her2 degradation after 24 hrs by high content screening	[PMID: 19552433]
AU565	IC₅₀	8 nM Compound: 2, 17-AAG	Inhibition of Hsp90 in human AU565 cells assessed as pERK degradation after 24 hrs by high content screening Inhibition of Hsp90 in human AU565 cells assessed as pERK degradation after 24 hrs by high content screening	[PMID: 19552433]
BGC-823	IC₅₀	847 nM Compound: 17-Aag	Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay	[PMID: 25277067]
BT-474	IC₅₀	0.01 μM Compound: 17-AAG	Antiproliferative activity against human BT474 cells by MTS assay Antiproliferative activity against human BT474 cells by MTS assay	[PMID: 17488003]
BT-474	GI₅₀	5 nM Compound: 3, 17-AAG	Growth inhibition of human BT474 cells assessed as ATP level after 4 days Growth inhibition of human BT474 cells assessed as ATP level after 4 days	[PMID: 19410458]
CNE-2	IC₅₀	3.03 μM Compound: 17-AAG	Cytotoxicity in human CNE-2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity in human CNE-2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33543615]
CNE2Z	IC₅₀	8.41 μM Compound: 17-AAG	Antiproliferative activity against human CNE2Z cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human CNE2Z cells assessed as cell growth inhibition by MTT assay	[PMID: 32527461]
DU-145	IC₅₀	0.282 μM Compound: 2; 17-AAG	Antiproliferative activity against human DU145 cells after 48 hrs by MTT assay Antiproliferative activity against human DU145 cells after 48 hrs by MTT assay	[PMID: 28073608]
DU-145	IC₅₀	68.3 μM Compound: 17-AAG	Cytotoxicity against DU145 cells after 72 hrs Cytotoxicity against DU145 cells after 72 hrs	[PMID: 17181154]
ECa-109 cell line	IC₅₀	1.1 μM Compound: Tanespimycin, 17-AAG	Cytotoxicity against human ECA109 cells after 48 hrs by MTT assay Cytotoxicity against human ECA109 cells after 48 hrs by MTT assay	[PMID: 23621840]
GES1	CC₅₀	7.94 μM Compound: 4; 17-AAG	Cytotoxicity against human GES1 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Cytotoxicity against human GES1 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 33189438]
HCC827	GI₅₀	56 nM Compound: 3, 17-AAG	Growth inhibition of human tarceva and iressa-resistant HCC827 cells assessed as ATP level after 4 days Growth inhibition of human tarceva and iressa-resistant HCC827 cells assessed as ATP level after 4 days	[PMID: 19410458]
HCT-116	GI₅₀	0.16 μM Compound: 1b, 17-AAG	Growth inhibition of human HCT116 cells after 24 hrs by SRB assay Growth inhibition of human HCT116 cells after 24 hrs by SRB assay	[PMID: 18020435]
HCT-116	GI₅₀	0.34 μM Compound: 1; 17-AAG	Antiproliferative activity against human HCT116 cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay Antiproliferative activity against human HCT116 cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay	[PMID: 33934008]
HCT-116	GI₅₀	0.34 μM Compound: III; 17AAG	Antiproliferative activity against human HCT116 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay Antiproliferative activity against human HCT116 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay	[PMID: 31655430]
HCT-116	IC₅₀	202 nM Compound: Tanespimycin, 17-AAG	Cytotoxicity against human HCT116 cells after 72 hrs Cytotoxicity against human HCT116 cells after 72 hrs	[PMID: 19231864]
HCT-116	IC₅₀	56.5 nM Compound: 17-AAG	Growth inhibition of human HCT116 cells after 24 hrs by [3H]thymidine uptake assay Growth inhibition of human HCT116 cells after 24 hrs by [3H]thymidine uptake assay	[PMID: 20014866]
HCT-15	IC₅₀	1487 nM Compound: 2, 17-AAG	Antiproliferative activity against human HCT15 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human HCT15 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
HeLa	IC₅₀	> 1000 μM Compound: III; 17AAG	Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate measured after 30 mins by fluorescence assay Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate measured after 30 mins by fluorescence assay	[PMID: 31655430]
HeLa	IC₅₀	0.2 μM Compound: 17-AAG	Antiproliferative activity against human HeLa cells after 72 hrs by SRB assay Antiproliferative activity against human HeLa cells after 72 hrs by SRB assay	[PMID: 27266997]
HeLa	IC₅₀	108.2 μM Compound: 17-AAG	Cytotoxicity against HeLa cells after 72 hrs Cytotoxicity against HeLa cells after 72 hrs	[PMID: 17181154]
HeLa	IC₅₀	128 nM Compound: 17-Aag	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay Cytotoxicity against human HeLa cells after 72 hrs by MTT assay	[PMID: 25277067]
HeLa	IC₅₀	19.4 μM Compound: 17-AAG	Cytotoxicity in human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity in human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33543615]
Hep 3B2	GI₅₀	0.08 μM Compound: 1; 17-AAG	Antiproliferative activity against human Hep3B cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay Antiproliferative activity against human Hep3B cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay	[PMID: 33934008]
HepG2	IC₅₀	0.32 μM Compound: 17-AAG	Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition by MTT assay	[PMID: 32527461]
HepG2	IC₅₀	0.33 μM Compound: 4; 17-AAG	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay	[PMID: 33189438]
HepG2	IC₅₀	8 μM Compound: 17-AAG	Cytotoxicity in human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity in human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33543615]
HepG2	IC₅₀	91 nM Compound: 17-Aag	Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 25277067]
HT-29	IC₅₀	0.1 nM Compound: 2, 17-AAG	Antiproliferative activity against human HT-29 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human HT-29 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
HUVEC	GI₅₀	< 0.1 μM Compound: 1; 17-AAG	Antiproliferative activity against human HUVEC cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay Antiproliferative activity against human HUVEC cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay	[PMID: 33934008]
HUVEC	IC₅₀	282 nM Compound: 17-Aag	Cytotoxicity against HUVEC cells after 72 hrs by MTT assay Cytotoxicity against HUVEC cells after 72 hrs by MTT assay	[PMID: 25277067]
K562	IC₅₀	0.15 μM Compound: 1, 17-AAG	Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by trypan blue exclusion assay Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by trypan blue exclusion assay	[PMID: 24565573]
K562	IC₅₀	126 nM Compound: 2, 17-AAG	Antiproliferative activity against human K562 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human K562 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
K562	GI₅₀	48 nM Compound: 3, 17-AAG	Growth inhibition of human K562 cells assessed as ATP level after 4 days Growth inhibition of human K562 cells assessed as ATP level after 4 days	[PMID: 19410458]
L02	CC₅₀	11.65 μM Compound: 4; 17-AAG	Cytotoxicity against human L02 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 33189438]
L02	IC₅₀	99 nM Compound: 17-Aag	Cytotoxicity against human HL7702 cells after 72 hrs by MTT assay Cytotoxicity against human HL7702 cells after 72 hrs by MTT assay	[PMID: 25277067]
LNCaP	IC₅₀	0.16 μM Compound: 17-AAG	Cytotoxicity against human LNCAP cells after 72 hrs by MTT assay Cytotoxicity against human LNCAP cells after 72 hrs by MTT assay	[PMID: 25105924]
LNCaP	IC₅₀	82 nM Compound: 2, 17-AAG	Antiproliferative activity against human LNCAP cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human LNCAP cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
LoVo	IC₅₀	0.26 μM Compound: 4; 17-AAG	Antiproliferative activity against human LoVo cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay Antiproliferative activity against human LoVo cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay	[PMID: 33189438]
MCF7	IC₅₀	0.01 μM Compound: 17-AAG	Antiproliferative activity against human MCF7 cells by MTS assay Antiproliferative activity against human MCF7 cells by MTS assay	[PMID: 17488003]
MCF7	IC₅₀	0.029 μM Compound: 17-AAG	Antiproliferative activity against human MCF7 cells measured after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells measured after 48 hrs by MTT assay	[PMID: 27153346]
MCF7	IC₅₀	0.09 μM Compound: 1b, 17-AAG	Antiproliferative activity against human MCF7 cells assessed as cell viability after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 21920765]
MCF7	IC₅₀	0.192 μM Compound: 2; 17-AAG	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 28073608]
MCF7	IC₅₀	0.3 nM Compound: 2, 17-AAG	Antiproliferative activity against human MCF7 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human MCF7 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
MCF7	IC₅₀	5 nM Compound: 17-AAG	Antiproliferative activity against human MCF7 cells measured after 5 days by MTS assay Antiproliferative activity against human MCF7 cells measured after 5 days by MTS assay	[PMID: 27153346]
MCF7	IC₅₀	58 nM Compound: Tanespimycin, 17-AAG	Cytotoxicity against human MCF7 cells after 72 hrs Cytotoxicity against human MCF7 cells after 72 hrs	[PMID: 19231864]
MCF7	IC₅₀	662 nM Compound: Tanespimycin, 17-AAG	Cytotoxicity against human MCF7 cells after 72 hrs in presence of NQO1 inhibitor dicoumarol Cytotoxicity against human MCF7 cells after 72 hrs in presence of NQO1 inhibitor dicoumarol	[PMID: 19231864]
MDA-MB-231	GI₅₀	0.27 μM Compound: 1; 17-AAG	Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay	[PMID: 33934008]
MDA-MB-231	IC₅₀	0.28 μM Compound: 17-Aag	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 25277067]
MDA-MB-231	IC₅₀	0.28 μM Compound: 17-AAG	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 25105924]
MDA-MB-231	IC₅₀	0.52 μM Compound: 17-AAG	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay	[PMID: 27266997]
MDA-MB-231	IC₅₀	1.79 μM Compound: 17-AAG	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition by MTT assay	[PMID: 32527461]
MDA-MB-231	IC₅₀	194 nM Compound: 2, 17-AAG	Antiproliferative activity against human MDA-MB-231 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human MDA-MB-231 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
MDA-MB-468	IC₅₀	1.57 μM Compound: 17-AAG	Antiproliferative activity against human MDA-MB-468 cells measured after 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells measured after 48 hrs by MTT assay	[PMID: 27153346]
MDA-MB-468	IC₅₀	1500 nM Compound: Tanespimycin, 17-AAG	Cytotoxicity against NQ01-deficient human MDA468 cells after 72 hrs Cytotoxicity against NQ01-deficient human MDA468 cells after 72 hrs	[PMID: 19231864]
MDA-MB-468	GI₅₀	780 nM Compound: 3, 17-AAG	Growth inhibition of human MDA-MB-468 cells assessed as ATP level after 4 days Growth inhibition of human MDA-MB-468 cells assessed as ATP level after 4 days	[PMID: 19410458]
MRC5	CC₅₀	14.24 μM Compound: 4; 17-AAG	Cytotoxicity against human MRC5 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Cytotoxicity against human MRC5 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 33189438]
MV4-11	GI₅₀	11 nM Compound: 3, 17-AAG	Growth inhibition of human MV4-11 cells assessed as ATP level after 4 days Growth inhibition of human MV4-11 cells assessed as ATP level after 4 days	[PMID: 19410458]
NCI-H1299	IC₅₀	0.2 μM Compound: 17-AAG	Antiproliferative activity against human H1299 cells after 48 hrs by resazurin dye-based fluorescence assay Antiproliferative activity against human H1299 cells after 48 hrs by resazurin dye-based fluorescence assay	[PMID: 28426997]
NCI-H1975	GI₅₀	0.16 μM Compound: III; 17AAG	Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay	[PMID: 31655430]
NCI-H1975	GI₅₀	35 nM Compound: 3, 17-AAG	Growth inhibition of human tarceva and iressa-resistant NCI-H1975 cells assessed as ATP level after 4 days Growth inhibition of human tarceva and iressa-resistant NCI-H1975 cells assessed as ATP level after 4 days	[PMID: 19410458]
NCI-H460	IC₅₀	0.01 μM Compound: 17-AAG	Cytotoxicity against human NCI-H460 cells after 72 hrs Cytotoxicity against human NCI-H460 cells after 72 hrs	[PMID: 22538015]
NCI-H460	IC₅₀	255 nM Compound: 2, 17-AAG	Antiproliferative activity against human NCI-H460 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human NCI-H460 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
NCI-H596	IC₅₀	1600 nM Compound: Tanespimycin, 17-AAG	Cytotoxicity against NQ01-deficient human NCI-H596 cells after 72 hrs Cytotoxicity against NQ01-deficient human NCI-H596 cells after 72 hrs	[PMID: 19231864]
NCI-N87	GI₅₀	1 nM Compound: 3, 17-AAG	Growth inhibition of human NCI-N87 cells assessed as ATP level after 4 days Growth inhibition of human NCI-N87 cells assessed as ATP level after 4 days	[PMID: 19410458]
NCM460	CC₅₀	14.21 μM Compound: 4; 17-AAG	Cytotoxicity against human NCM460 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Cytotoxicity against human NCM460 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 33189438]
OVCAR-3	IC₅₀	0.48 μM Compound: 4; 17-AAG	Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay	[PMID: 33189438]
PANC-1	IC₅₀	3.21 μM Compound: 4; 17-AAG	Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay	[PMID: 33189438]
PC-3	IC₅₀	0.062 μM Compound: 17-AAG	Antiproliferative activity against human PC-3 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human PC-3 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay	[PMID: 32663707]
PC-3	IC₅₀	9 nM Compound: 2, 17-AAG	Antiproliferative activity against human PC3 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human PC3 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
SGC-7901	IC₅₀	> 10 μM Compound: 4; 17-AAG	Antiproliferative activity against human SGC-7901 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay Antiproliferative activity against human SGC-7901 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay	[PMID: 33189438]
SK-BR-3	EC₅₀	< 0.1 μM Compound: 1, 17-AAG	Inhibition of Hsp90alpha in human SKBR3 cells assessed as ErbB2 degradation by Western blot analysis Inhibition of Hsp90alpha in human SKBR3 cells assessed as ErbB2 degradation by Western blot analysis	[PMID: 21106457]
SK-BR-3	IC₅₀	0.038 μM Compound: 17-AAG	Antiproliferative activity against human SK-BR-3 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human SK-BR-3 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay	[PMID: 32663707]
SK-BR-3	EC₅₀	0.06 μM Compound: 1, 17-AAG	Inhibition of Hsp90alpha in human SKBR3 cells assessed as up-regulation of HSP70 protein by Western blot analysis Inhibition of Hsp90alpha in human SKBR3 cells assessed as up-regulation of HSP70 protein by Western blot analysis	[PMID: 21106457]
SK-BR-3	IC₅₀	27 nM Compound: 17-AAG	Cytotoxicity against human SKBR3 cells after 72 hrs by celltiter-Glo assay Cytotoxicity against human SKBR3 cells after 72 hrs by celltiter-Glo assay	[PMID: 15844961]
SK-BR-3	IC₅₀	33 nM Compound: 1b, 17-AAG	Cytotoxicity against human SKBR3 cells after 72 hrs by celltiter-glo assay Cytotoxicity against human SKBR3 cells after 72 hrs by celltiter-glo assay	[PMID: 19405528]
SK-BR-3	IC₅₀	410 nM Compound: Tanespimycin, 17-AAG	Cytotoxicity against human SKBR3 cells after 72 hrs in presence of NQO1 inhibitor dicoumarol Cytotoxicity against human SKBR3 cells after 72 hrs in presence of NQO1 inhibitor dicoumarol	[PMID: 19231864]
SK-BR-3	IC₅₀	44 nM Compound: Tanespimycin, 17-AAG	Cytotoxicity against human SKBR3 cells after 72 hrs Cytotoxicity against human SKBR3 cells after 72 hrs	[PMID: 19231864]
SK-MEL-5	IC₅₀	134 nM Compound: 2, 17-AAG	Antiproliferative activity against human SK-MEL-5 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human SK-MEL-5 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
SK-OV-3	IC₅₀	0.22 μM Compound: 17-AAG	Antiproliferative activity against human SK-OV-3 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human SK-OV-3 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay	[PMID: 32663707]
SK-OV-3	IC₅₀	240 nM Compound: Tanespimycin, 17-AAG	Cytotoxicity against human SKOV3 cells after 72 hrs Cytotoxicity against human SKOV3 cells after 72 hrs	[PMID: 19231864]
SMMC-7721	IC₅₀	0.19 μM Compound: 17-AAG	Antiproliferative activity against human SMMC7721 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human SMMC7721 cells assessed as cell growth inhibition by MTT assay	[PMID: 32527461]
SW480	IC₅₀	0.28 μM Compound: 17-AAG	Antiproliferative activity against human SW480 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human SW480 cells assessed as cell growth inhibition by MTT assay	[PMID: 32527461]
SW480	IC₅₀	572 nM Compound: 17-Aag	Cytotoxicity against human SW480 cells after 72 hrs by MTT assay Cytotoxicity against human SW480 cells after 72 hrs by MTT assay	[PMID: 25277067]
SW-620	IC₅₀	328 nM Compound: 2, 17-AAG	Antiproliferative activity against human SW620 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human SW620 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
U-87MG ATCC	IC₅₀	> 10 μM Compound: 17-AAG	Antiproliferative activity against human U-87 MG cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human U-87 MG cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay	[PMID: 32663707]

體外研究
(In Vitro)

Tanespimycin 導致 HER2、Akt 以及突變型和野生型 AR 的降解以及前列腺癌細胞的視網膜母細胞瘤依賴性 G1 期生長停滯。Tanespimycin 抑制前列腺癌細胞系，IC₅₀ 范圍為 25-45 nM (LNCaP，25 nM；LAPC-4，40 nM；DU-145，45 nM；和 PC-3，25 nM)^[1]。
Tanespimycin (0.1-1 μM) 誘導過表達 ErbB2 的乳腺癌細胞幾乎完全喪失 ErbB2^[2]。
Tanespimycin 抑制 CCA 細胞生長并誘導 G2/M 細胞周期停滯和凋亡，同時下調 Bcl-2、Survivin 和 Cyclin B1，上調 cleaved PARP^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

體內研究
(In Vivo)

Tanespimycin (25 -200 mg/kg，ip) 引起前列腺癌異種移植物中 AR、HER2 和 Akt 表達的劑量依賴性下降。Tanespimycin 以足以誘導 AR、HER2 和 Akt 降解的劑量進行處理，可劑量依賴性地抑制雄激素依賴性和非依賴性前列腺癌異種移植物的生長，且無毒性^[1]。
Tanespimycin (60 mg/kg) 和 Rapamycin (30 mg/kg) 通過尾靜脈注射抑制 A549 和 MDA-MB-231 腫瘤生長并影響 MDA-MB-231 荷瘤動物的腫瘤治愈^[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

585.69

Formula

C₃₁H₄₃N₃O₈

CAS 號

75747-14-7

性狀

固體

顏色

Purple to purplish red

中文名稱

坦螺旋霉素

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性數據

細胞實驗：

DMSO 中的溶解度 : 50 mg/mL (85.37 mM; 超聲助溶; 吸濕的 DMSO 對產品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液

濃度溶劑體積質量	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

查看完整儲備液配制表

* 請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲存時，請在6個月內使用，-20°C儲存時，請在1個月內使用。

摩爾計算器
稀釋計算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動物實驗：

請根據您的實驗動物和給藥方式選擇適當的溶解方案。

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結果的可靠性，澄清的儲備液可以根據儲存條件，適當保存；體內實驗的工作液，建議您現用現配，當天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現沉淀、析出現象，可以通過加熱和/或超聲的方式助溶

方案一

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (8.54 mM); 澄清溶液

此方案可獲得 ≥ 5 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 50.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液中，混合均勻。
2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
方案二

請依序添加每種溶劑： 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (8.54 mM); 澄清溶液

此方案可獲得 ≥ 5 mg/mL（飽和度未知）的澄清溶液，此方案實驗周期在半個月以上的動物實驗酌情使用。
以 1 mL 工作液為例，取 100 μL 50.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中，混合均勻。
方案三

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.62 mg/mL (2.77 mM); 澄清溶液

此方案可獲得 ≥ 1.62 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 16.2 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水定容至 1 mL。
生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。

以下溶解方案，請直接配制工作液。建議現用現配，在短期內盡快用完。以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現沉淀、析出現象，可以通過加熱和/或超聲的方式助溶。

方案一

請依序添加每種溶劑： 50% PEG300 50% Saline
Solubility: 10 mg/mL (17.07 mM); 懸濁液; 超聲助溶
方案二

請依序添加每種溶劑： 15% Cremophor EL 85% Saline
Solubility: 5 mg/mL (8.54 mM); 懸濁液; 超聲助溶

動物溶解方案計算器

請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

每只動物的給藥體積

μL

動物數量

只

由于實驗過程有損耗，建議您多配一只動物的量

請輸入您的動物體內配方組成：

DMSO +

Tween-80 +

Saline

如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。

方案所需 助溶劑 包括：DMSO，，均可在 MCE 網站選購。，Tween 80，均可在 MCE 網站選購。

計算結果

工作液所需濃度 : mg/mL

儲備液配制方法 : mg 藥物溶于 μL DMSO（母液濃度為 mg/mL）。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

您所需的儲備液濃度超過該產品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術支持聯系。

動物實驗體內工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。

連續(xù)給藥周期超過半月以上，請謹慎選擇該方案。

請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱（超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。

純度 & 產品資料

純度: 99.01%

選擇批次：

Data Sheet (647 KB) SDS (393 KB)

COA (196 KB) LCMS (96 KB)

產品使用指南 (1538 KB)

參考文獻

[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. [Content Brief]

[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 [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

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.
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.
參考文獻	[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. [Content Brief] [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 [Content Brief] [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. [Content Brief] [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. [Content Brief] [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. [Content Brief] [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. [Content Brief]

Tanespimycin 相關分類

完整儲備液配制表

可選溶劑	濃度溶劑體積質量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7074 mL	8.5369 mL	17.0739 mL	42.6847 mL
	5 mM	0.3415 mL	1.7074 mL	3.4148 mL	8.5369 mL
	10 mM	0.1707 mL	0.8537 mL	1.7074 mL	4.2685 mL
	15 mM	0.1138 mL	0.5691 mL	1.1383 mL	2.8456 mL
	20 mM	0.0854 mL	0.4268 mL	0.8537 mL	2.1342 mL
	25 mM	0.0683 mL	0.3415 mL	0.6830 mL	1.7074 mL
	30 mM	0.0569 mL	0.2846 mL	0.5691 mL	1.4228 mL
	40 mM	0.0427 mL	0.2134 mL	0.4268 mL	1.0671 mL
	50 mM	0.0341 mL	0.1707 mL	0.3415 mL	0.8537 mL
	60 mM	0.0285 mL	0.1423 mL	0.2846 mL	0.7114 mL
	80 mM	0.0213 mL	0.1067 mL	0.2134 mL	0.5336 mL

Help & FAQs

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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Tanespimycin (Synonyms: 坦螺旋霉素; 17-AAG; NSC 330507; CP 127374)

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MCE 顧客使用本產品發(fā)表的 46 篇科研文獻

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