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17-(allylamino)-17-demethoxygeldanamycin (17AAG)

Subscribe to New Research on 17-(allylamino)-17-demethoxygeldanamycin

an aminoquinone macrocyclic compound; shares the ability of geldanamycin to bind to heat shock protein 90 and GRP94; IPI-504 is the hydroquinone chloride salt which is more water soluble; structure in first source

Also Known As:

17AAG; 17-(allylamino)-17-demethoxy-geldanamycin; 17-AAG; 17-allyl-aminogeldanamycin; 17-allylamino-17-demethoxygeldanamycin; 17-allylamino-17-demethoxygeldanamycin hydroquinone; 17-allylamino-17-demethoxygeldanamycin hydroquinone salt; 17-allylamino-geldanamycin; 17-allylaminogeldanamycin; IPI 504; IPI-504; IPI504; NSC 330507; NSC-330507; retaspimycin hydrochloride; tanespimycin; ((4E,6E,8S,9S,10E,12S,13R,14S,16R)-13-hydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-19-(prop-2-enylamino)-2-azabicyclo(16.3.1)docosa-4,6,10,18,21-pentaen-9-yl) carbamate

Networked: 409 relevant articles (37 outcomes, 107 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Experts

1.	Rosen, Neal: 22 articles (04/2012 - 02/2002)
2.	Workman, Paul: 20 articles (05/2014 - 01/2002)
3.	Solit, David B: 17 articles (04/2012 - 02/2002)
4.	Erlichman, Charles: 12 articles (08/2015 - 02/2005)
5.	Normant, Emmanuel: 12 articles (11/2013 - 07/2006)
6.	Ivy, S Percy: 11 articles (04/2012 - 05/2005)
7.	Egorin, Merrill J: 9 articles (04/2012 - 06/2003)
8.	Neckers, Len: 8 articles (01/2013 - 02/2003)
9.	Scher, Howard I: 8 articles (07/2012 - 05/2002)
10.	Banerji, Udai: 7 articles (02/2012 - 11/2003)

Related Diseases

1.	Neoplasms (Cancer) 05/15/2005 - "Both 17-AAG and EC5 inhibited tumor cell proliferation effectively, but EC5 was more potent, with IC(50) below 200 nmol/L in most cell lines tested, including several lines that were resistant to 17-AAG. " 10/14/2003 - "Whereas 17-allylamino-17-demethoxygeldanamycin only modestly delayed the growth of established mammary tumors in WT mice for Id, tumor suppression was dramatically more effective in an Id1- or Id3-deficient background. " 04/01/2010 - "Compared to intravenous (i.v.) application, tumor uptake was significantly improved with intratumoral injection of (131)I-17-AAG and competitively reduced with preinjection of unlabeled 17-AAG. " 01/01/2008 - "DBM2 cells, which were derived from the DBTRG-05MG cell line were used to test the efficacy of 17AAG for treatment of intracranial tumors. " 06/28/2015 - "These studies demonstrate that polypeptide-based nanogels can serve as novel nanocarriers for encapsulating 17-AAG along with other chemotherapeutics, providing an opportunity to overcome solubility issues and thereby exploit its full potential as an anti-cancer agent."
2.	Breast Neoplasms (Breast Cancer) 06/01/2002 - "These findings suggest that 17-AAG may be useful for the treatment of breast cancer cells with high levels of HER2. " 02/01/2012 - "Based on these results, we do not recommend further study of 17-AAG at this dosing schedule or in unselected breast cancer patients." 02/01/2012 - "We conducted a phase II study of 17-AAG 220 mg/m(2) on days 1, 4, 8, and 11 every 21 days in patients with metastatic and locally advanced breast cancer. " 02/01/2012 - "A phase II study of 17-allylamino-17-demethoxygeldanamycin in metastatic or locally advanced, unresectable breast cancer." 02/01/2011 - "Tanespimycin represents a promising new agent for the treatment of relapsed/refractory MM. Results of ongoing and future trials will determine the role of tanespimycin both in MM and other malignancies, including breast cancer."
3.	Glioma (Gliomas) 04/01/2009 - "Efficacy of the HSP90 inhibitor 17-AAG in human glioma cell lines and tumorigenic glioma stem cells." 12/01/2014 - "These findings suggest that targeting Hsp90 by IPI-504 has the potential to become an active therapeutic strategy in gliomas in a selective group of patients, but further research into combination therapies is still needed. " 12/01/2014 - "Profiling Hsp90 differential expression and the molecular effects of the Hsp90 inhibitor IPI-504 in high-grade glioma models." 01/01/2013 - "Can RNAi-mediated hsp90α knockdown in combination with 17-AAG be a therapy for glioma?" 08/01/2009 - "Individually, 17-AAG and olaparib had modest, replication-dependent radiosensitizing effects on T98G glioma cells. "
4.	Pancreatic Neoplasms (Pancreatic Cancer) 10/01/2008 - "This study aimed to assess the antitumor activity of the Hsp90 inhibitor, IPI-504, in pancreatic cancer and to determine the biological effects of the agent. " 03/01/2011 - "The intracellular concentrations of 17AAG and 17AAGH₂ were measured in human pancreatic cancer cells, and it was observed that larger amounts of 17AAG and 17AAGH₂ could be detected in cells with catalytically active NQO1 compared with cells lacking NQO1 activity or cells pretreated with ES936. " 03/01/2011 - "17AAG induced substantial growth inhibition in human pancreatic cancer cell lines expressing NQO1. " 01/01/2011 - "These findings provide a rationale for further evaluation of broccoli/broccoli sprout preparations combined with 17-AAG for better efficacy and lower dose-limiting toxicity in pancreatic cancer." 10/04/2010 - "Western blotting showed that 17-AAG caused a 2- to 3-fold transient activation of MEK/ERK signaling in pancreatic cancer cells. "
5.	Acute Myeloid Leukemia (Acute Myelogenous Leukemia) 09/01/2012 - "17-AAG preferentially induced apoptosis and eliminated the colony formation capacity of mouse lymphoma CSCs and human acute myeloid leukemia (AML) CSCs. " 02/15/2005 - "Finally, cotreatment with LBH589 and 17-AAG also induced more apoptosis of IM-resistant primary CML-BC and acute myeloid leukemia (AML) cells (with activating mutation of FLT-3) than treatment with either agent alone." 07/01/2003 - "Here, we demonstrate that treatment of the human acute myeloid leukemia HL-60 cells with 17-AAG attenuates the intracellular levels of a number of Hsp-90 client proteins, including Akt, c-Raf-1, and c-Src. " 04/01/2006 - "The ability of 17-AAG to enhance the antileukemia activity of ATO was further demonstrated in primary leukemia cells isolated from patients with acute myeloid leukemia and chronic lymphocytic leukemia, including cells from refractory patients. " 09/01/2008 - "In addition, cotreatment with 17-AAG and tubacin augmented the loss of survival of K562 cells and viability of primary acute myeloid leukemia (AML) and chronic myeloid leukemia (CML) samples. "

Related Drugs and Biologics

1.	Heat-Shock Proteins (Heat-Shock Protein)
2.	geldanamycin
3.	trastuzumab (Herceptin)
4.	Phosphotransferases (Kinase)
5.	Hormones
6.	Rifabutin (Ansamycin)
7.	Paclitaxel (Taxol)
8.	Cyclin D1
9.	lapatinib (GW572016)
10.	polyglutamine

Related Therapies and Procedures

1.	Heterologous Transplantation (Xenotransplantation)
2.	Radiotherapy
3.	Drug Therapy (Chemotherapy)
4.	Castration
5.	Molecular Targeted Therapy