17-AAG

Modify Date: 2024-01-02 13:15:11

17-AAG structure	Common Name	17-AAG
	CAS Number	75747-14-7	Molecular Weight	585.688
	Density	1.2±0.1 g/cm3	Boiling Point	797.8±60.0 °C at 760 mmHg
	Molecular Formula	C₃₁H₄₃N₃O₈	Melting Point	201-203ºC
	MSDS	USA	Flash Point	436.3±32.9 °C

Use of 17-AAG

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.

Name	tanespimycin
Synonym	More Synonyms

Description	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.
Related Catalog	Signaling Pathways >> Autophagy >> Autophagy Signaling Pathways >> Cell Cycle/DNA Damage >> HSP Signaling Pathways >> Metabolic Enzyme/Protease >> HSP Signaling Pathways >> Autophagy >> Mitophagy Research Areas >> Cancer
Target	HSP90:5 nM (IC50) Mitophagy Autophagy
In Vitro	17-AAG causes the degradation of HER2, Akt, and both mutant and wild-type AR and the retinoblastoma-dependent G1 growth arrest of prostate cancer cells. 17-AAG 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]. Combination of 17-AAG (10 nM) and Trastuzumab induces more effective ErbB2-degradation. 17-AAG (0.1-1 μM) induces a nearly complete loss of ErbB2 on ErbB2-overexpressing breast cancer cells[2]. 17-AAG 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].
In Vivo	17-AAG (25-200 mg/kg, i.p.) causes a dose-dependent decline in AR, HER2, and Akt expression in prostate cancer xenografts. 17-AAG 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]. 17-AAG (60 mg/kg) with paclitaxel (60 mg/kg) and rapamycin (30 mg/kg) inhibits A549 and MDA-MB-231 tumor growth far more potently than paclitaxel-containing micelles and effected tumor cures in MDA-MB-231 tumor-bearing animals by tail vein injection[4].
Cell Assay	For the Alamar Blue proliferation assay, 2-4×103 cells are plated in 96-well plates. Later (48 h), cells are treated with 17-AAG 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 17-AAG 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.
Animal Admin	17-AAG 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 17-AAG 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.
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. A combination of Trastuzumab and 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.

Density	1.2±0.1 g/cm3
Boiling Point	797.8±60.0 °C at 760 mmHg
Melting Point	201-203ºC
Molecular Formula	C₃₁H₄₃N₃O₈
Molecular Weight	585.688
Flash Point	436.3±32.9 °C
Exact Mass	585.304993
PSA	166.28000
LogP	2.68
Vapour Pressure	0.0±6.4 mmHg at 25°C
Index of Refraction	1.566

Personal Protective Equipment	Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
Hazard Codes	Xi
Risk Phrases	36/37/38
Safety Phrases	22-24/25-36-26
RIDADR	NONH for all modes of transport
WGK Germany	3
HS Code	29419090

Precursor 2
CAS#:107-11-9 Allylamine CAS#:30562-34-6 Geldanamycin
DownStream 2
CAS#:857402-23-4 Retaspimycin CAS#:64202-81-9 17-Aminodemetho...

Interactome analysis of the human respiratory syncytial virus RNA polymerase complex identifies protein chaperones as important cofactors that promote L-protein stability and RNA synthesis.

J. Virol. 89(2) , 917-30, (2015)

The human respiratory syncytial virus (HRSV) core viral RNA polymerase comprises the large polymerase protein (L) and its cofactor, the phosphoprotein (P), which associate with the viral ribonucleopro...

HGUE-C-1 is an atypical and novel colon carcinoma cell line.

BMC Cancer 15 , 240, (2015)

Colorectal carcinoma is a common cause of cancer. Adjuvant treatments include: 5-fluorouracil administered together with folinic acid, or more recently, oral fluoropyrimidines such as capecitabine, in...

Comparative Study of 17-AAG and NVP-AUY922 in Pancreatic and Colorectal Cancer Cells: Are There Common Determinants of Sensitivity?

Transl. Oncol. 7(5) , 590-604, (2014)

The use of heat shock protein 90 (Hsp90) inhibitors is an attractive antineoplastic therapy. We wanted to compare the effects of the benzoquinone 17-allylamino-17-demethoxygeldanamycin (17-AAG, tanesp...

17-AAG,17AAG

17-AG

2-azabicyclo[16.3.1]docosa-2,4,6,10,18,21-hexaene-20,22-dione, 3,13-dihydroxy-9-(hydroxyiminomethoxy)-8,14-dimethoxy-4,10,12,16-tetramethyl-19-(2-propen-1-ylamino)-, (2E,4E,6Z,8S,9S,10E,12S,13R,14S,16R)-

17-AGG

17-AAG (Tanespimycin)

KOS 953

(4E,6Z,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

MFCD04973892

2-Azabicyclo[16.3.1]docosa-4,6,10,18,21-pentaene-3,20,22-trione, 9-[(aminocarbonyl)oxy]-13-hydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-19-(2-propen-1-ylamino)-, (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-

Telatinib

(4E,6Z,8S,9S,10E,12S,13R,14S,16R)-13-hydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-19-(prop-2-en-1-ylamino)-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl carbamate

[3H]-17-AAG

17-demethoxygeldanamycin

17-allylamino-17-demethoxygeldanamycin

Tanespimycin

17-AAG

Gld-36

17-AAG (KOS953)

Shanghai Jizhi Biochemical Technology Co., Ltd
China
Product Name: 17-AAG
Price: ￥848.0/25mg ￥2038.0/100mg
Purity: 98.0%
Stocking Period: 1 Day
Contact: Liu jia

DC Chemicals Limited
China
Product Name: 17-AAG
Price: $800.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: 17-Aag
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

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Price: $79/10mM*1mLinDMSO

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17-AAG

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