17-AAG

HSP90 inhibitor



BML-EI308-0001	1 mg	182.00 USD

Replaces Prod. #: ALX-380-091

17-AAG is a less toxic and more stable analog of geldanamycin. It is 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 Akt activation and expression in tumors and synergizes with a number of antitumor agents such as taxol, cisplatin, and UCN-014. 17-AAG causes the inactivation, destabilization and eventual degradation of HIF-1α. Inhibitor of telomerase activity. Inducer of apoptosis with antitumor activity.

Alternative Name:	17-(Allylamino)-17-desmethoxygeldanamycin

Identity:	Identity determined by ¹H-NMR.

Formula:	C₃₁H₄₃N₃O₈

MW:	585.7

Purity:	≥98% (TLC)

Appearance:	Red to dark red powder.

CAS:	75747-14-7

Source/Host:	Semisynthetic derivative from geldanamycin.

Solubility:	Soluble in DMSO (>20mg/ml) or 100% ethanol (10mg/ml).

Long Term Storage:	-20°C

Handling:	Protect from light.

Background / Technical Information:	Please click here for the comprehensive product data sheet. Replacement for ADI-HPK-101

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Product Literature References

17-AAG induces cytoplasmic alpha-synuclein aggregate clearance by induction of autophagy: M. Riedel, et al.; PLos One 5, e8753 (2010), Abstract; Full Text

An in vitro and in vivo study of the combination of the heat shock protein inhibitor 17-allylamino-17-demethoxygeldanamycin and carboplatin in human ovarian cancer models: U. Banerji, et al.; Cancer Chemother. Pharmacol. 62, 769 (2008), Abstract;

HSP90 inhibitor 17AAG causes apoptosis in ATRA-resistant acute promyelocytic leukemia cells: P.N. Meyer, et al.; Leuk. Res. 32, 143 (2008), Abstract;

Drugging the cancer chaperone HSP90: Combinatorial therapeutic exploitation of oncogene addiction and tumor stress: P. Workman, et al.; Ann. N.Y. Acad. Sci. 1113, 202 (2007), Abstract;

Intratumor injection of the Hsp90 inhibitor 17AAG decreases tumor growth and induces apoptosis in a prostate cancer xenograft model: C.R. Williams, et al.; J. Urol. 178, 1528 (2007), Abstract;

Phase I and pharmacodynamic study of 17-(allylamino)-17-demethoxygeldanamycin in adult patients with refractory advanced cancers: R.K. Ramanathan, et al.; Clin. Cancer Res. 13, 1769 (2007), Abstract;

Rituximab and 17-allylamino-17-demethoxygeldanamycin induce synergistic apoptosis in B-cell chronic lymphocytic leukaemia: A.J. Johnson, et al.; Br. J. Haematol. 139, 837 (2007), Abstract;

Synergism between etoposide and 17-AAG in leukemia cells: critical roles for Hsp90, FLT3, topoisomerase II, Chk1, and Rad51: Q. Yao, et al.; Clin. Cancer Res. 13, 1591 (2007), Abstract; Full Text

Chaperoning oncogenes: HSP90 as a target of geldanamycin: L. Neckers; Handb. Exp. Pharmacol. 259 (2006), Abstract;

Quantitative effects on c-Jun N-terminal protein kinase signaling determine synergistic interaction of cisplatin and 17-allylamino-17-demethoxygeldanamycin in colon cancer cell lines: I.A. Vasilevskaya, et al.; Mol. Pharmacol. 65, 235 (2004), Abstract;

A high-affinity conformation of Hsp90 confers tumour selectivity on Hsp90 inhibitors: A. Kamal, et al.; Nature 425, 407 (2003), Abstract;

ErbB2 degradation mediated by the co-chaperone protein CHIP: P. Zhou, et al.; J. Biol. Chem. 278, 13829 (2003), Abstract;

Geldanamycin and its 17-allylamino-17-demethoxy analogue antagonize the action of Cisplatin in human colon adenocarcinoma cells: differential caspase activation as a basis for interaction: I.A. Vasilevskaya, et al.; Cancer Res. 63, 3241 (2003), Abstract;

Inhibition of heat shock protein 90 function down-regulates Akt kinase and sensitizes tumors to Taxol: D.B. Solit, et al.; Cancer Res. 63, 2139 (2003), Abstract;

Inhibition of telomerase activity by geldanamycin and 17-allylamino, 17-demethoxygeldanamycin in human melanoma cells: R. Villa, et al.; Carcinogenesis 24, 851 (2003), Abstract;

Synergistic antileukemic interactions between 17-AAG and UCN-01 involve interruption of RAF/MEK- and AKT-related pathways: W. Jia, et al.; Blood 102, 1824 (2003), Abstract;

Disruption of the EF-2 kinase/Hsp90 protein complex: a possible mechanism to inhibit glioblastoma by geldanamycin: J. Yang, et al.; Cancer Res. 61, 4010 (2001), Abstract; Full Text

Enhancement of paclitaxel-mediated cytotoxicity in lung cancer cells by 17-allylamino geldanamycin: in vitro and in vivo analysis: D.M. Nguyen, et al.; Ann. Thorac. Surg. 72, 371 (2001), Abstract;

Geldanamycin and its analogue 17-allylamino-17-demethoxygeldanamycin lowers Bcr-Abl levels and induces apoptosis and differentiation of Bcr-Abl-positive human leukemic blasts: R. Nimmanapalli, et al.; Cancer Res. 61, 1799 (2001), Abstract; Full Text

Inhibition of heat shock protein 90 function by ansamycins causes the morphological and functional differentiation of breast cancer cells: P.N. Munster, et al.; Cancer Res. 61, 2945 (2001), Abstract; Full Text

Gene expression profiling of human colon cancer cells following inhibition of signal transduction by 17-allylamino-17-demethoxygeldanamycin, an inhibitor of the hsp90 molecular chaperone: P.A. Clarke, et al.; Oncogene 19, 4125 (2000), Abstract;

The benzoquinone ansamycin 17-allylamino-17-demethoxygeldanamycin binds to HSP90 and shares important biologic activities with geldanamycin: T.W. Schulte & L.M. Neckers; Cancer Chemother. Pharmacol. 42, 273 (1998), Abstract;

Inhibition of the oncogene product p185erbB-2 in vitro and in vivo by geldanamycin and dihydrogeldanamycin derivatives: R.C. Schnur, et al.; J. Med. Chem. 38, 3806 (1995), Abstract;