17-AAGA potent Hsp90 inhibitor for tumor cells

17-AAG (CAS 75747-14-7)

17-AAG | CAS 75747-14-7 is rated 5.0 out of 5 by 2.
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Synonym: 17-(Allylamino)-17-desmethoxygeldanamycin
Application: A potent Hsp90 inhibitor for tumor cells
CAS Number: 75747-14-7
Purity: ≥98%
Molecular Weight: 585.69
Molecular Formula: C31H43N3O8
* Refer to Certificate of Analysis for lot specific data (including water content).
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17-AAG is a less toxic and more stable analog of geldanamycin. It acts an Hsp90 inhibitor that displays a 100-fold higher affinity for Hsp90 derived from tumor cells compared to Hsp90 from normal cells. 17-AAG inhibits Akt1 (Akt) activation and expression in tumors and synergizes with a number of anti tumor agents such as taxol2, cisplatin3, and UCN-014. 17-AAG causes the inactivation, destabilization and eventual degradation of HIF-1α5. 17-AAG is an inhibitor of K-Ras and N-Ras.


References

1. Kamal A., et al. 2003. Nature. 425: 407-410. PMID: 14508491
2. Solit, D.B., et al. 2003. Cancer Res. 63: 2139-2144. PMID: 12727831
3. Vasilevskaya, I.A., et al. 2004. Mol. Pharmacol. 65: 235-243. PMID: 14722256
4. Jia, W., et al. 2003. Blood. 102: 1824-1832. PMID: 12738674
5. Neckers, L. 2003. Current Med. Chem. 10: 733-739. PMID: 12678776

Physical State :
Solid
Solubility :
Soluble in DMSO (≥20 mg/ml at 25° C), methanol (10 mg/ml), chloroform (10 mg/ml yielding a clear purple solution), water (<1 mg/ml at 25° C), and ethanol (≥5 mg/ml at 25° C).
Storage :
Store at -20° C
Boiling Point :
~797.8° C at 760 mmHg (Predicted)
Density :
~1.2 g/cm3 (Predicted)
Refractive Index :
n20D 1.57
IC50 :
Hsp90: EC5050 = 7.2 µM; SKBR3: IC50 = 4.1 nM; MCF7 cells: IC50 = 5.2 nM; cancer cells of erbB-1, erbB-2: EC5050 = 45 nM; mutant p53: EC5050 = 62 nM; Raf-1: EC5050 = 80 nM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
6505803
MDL Number :
MFCD04973892
SMILES :
C[C@H]1C[C@@H]([C@@H]([C@H](/C=C(/[C@@H]([C@H](/C=C\\C=C(\\C(=O)NC2=CC(=O)C(=C(C1)C2=O)NCC=C)/C)OC)OC(=O)N)\\C)C)O)OC

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Certificate of Analysis

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17-AAG  Product Citations

See how others have used 17-AAG. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 10 total

PMID: # 28911204  Medina-Carmona, E. et al. 2017. Human molecular genetics. 26: 3531-3544.

PMID: # 29145196  Centrone, M. et al. 2017. Cell. Physiol. Biochem. 44: 515-531.

PMID: # 27075590  Mohammadi, A. et al. 2016. Inflammation.

PMID: # 27894402  Mohammadi, A.|Yaghoobi, MM.|GholamhoseynianNajar, A.|Kalantari-Khandani, B.|Sharifi, H.|Saravani, M.| et al. 2016. Cell. Mol. Biol. (Noisy-le-grand). 62: 62-67.

PMID: # 25196280  Wang, B. et al. 2014. Experimental cell research. 328: 379-87.

PMID: # 24869908  Kim, H. et al. 2014. Molecular medicine (Cambridge, Mass.). 20: 270-9.

PMID: # 25263741  Taniguchi, H. et al. 2014. Cancer science. 105: 1601-8.

PMID: # 24317089  Born, EJ. et al. 2013. Blood cancer journal. 3: e167.

PMID: # 22085491  Sobhan, PK. et al. 2012. Cancer Lett. 317: 78-88.

PMID: # 21976548  Fiskus, W. et al. 2011. Clinical cancer research : an official journal of the American Association for Cancer Research. 17: 7347-58.

Citations 1 to 10 of 10 total

What is the storage once the compound is dissolved in DMSO? And what is the relative stability?

Asked by: two2igm05
Thank you for your question. For 17-AAG, sc-200641, we recommend that stock solutions, once prepared, be stored aliquoted in tightly sealed vials at -20&deg;C or below and used within 1 month. Wherever possible, solutions should be made up and used on the same day.
Answered by: TechService7
Date published: 2016-12-21
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Rated 5 out of 5 by from The quality of this chemical was very good The quality of this chemical was very good for the price.
Date published: 2015-09-10
Rated 5 out of 5 by from A decrease in EGFR expression was observed A decrease in EGFR expression was observed by WB when treating T98G cells with 17-AAG. -SCBT QC
Date published: 2015-01-27
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