17-AAG |  | | SYNONYMS | 17-(Allylamino)-17-desmethoxygeldanamycin | | | | PRODUCT LINE | Natural Products / Antibiotics | | | | PRODUCT FAMILIES | Antitumor Antibiotics | | | | | Ordering Information | | | Product Numbers | Format | Size | Unit Price | Quantity | | | ALX-380-091-C100 |
|
100 µg | | | | | ALX-380-091-M001 |
|
1 mg | | | | | | |
| | | Product Specification | | |
| FORMULA: | C31H43N3O8 | | | | | |
| MW: | 585.7 | | | | | |
| CAS NUMBER: | 75747-14-7 | | | | | |
| SOURCE/HOST: | Semisynthetic derivative from geldanamycin. | | | | | |
| PURITY: | ≥97% | | | | | |
| APPEARANCE: | Red to dark red powder. | | | | | |
| SOLUBILITY: | Soluble in DMSO (10mg/ml) or methanol (10mg/ml). | | | | | |
| SHIPPING: | AMBIENT | | | | | |
| LONG TERM STORAGE: | -20°C | | | | | |
| HANDLING: | Protect from light. | | | | | | Product Description | Potent, less toxic derivative of geldanamycin (Prod. No. ALX-380-054). Inhibits the essential ATPase activity of HSP90. Inhibitor of telomerase activity. Inducer of apoptosis with antitumor activity. |
| | | Product Specific Literature References | 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
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
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
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) Full Text; http://cancerres.aacrjournals.org/cgi/content/full/61/5/1799
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) Full Text; http://cancerres.aacrjournals.org/cgi/content/full/61/7/2945
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) Full Text; http://cancerres.aacrjournals.org/cgi/content/full/61/10/4010
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
ErbB2 degradation mediated by the co-chaperone protein CHIP: P. Zhou, et al.; J. Biol. Chem. 278, 13829 (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
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
A high-affinity conformation of Hsp90 confers tumour selectivity on Hsp90 inhibitors: A. Kamal, et al.; Nature 425, 407 (2003) Abstract
Chaperoning oncogenes: HSP90 as a target of geldanamycin: L. Neckers; Handb. Exp. Pharmacol. 259 (2006) 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
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) Full Text; http://clincancerres.aacrjournals.org/cgi/reprint/13/5/1591.pdf
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
HSP90 inhibitor 17AAG causes apoptosis in ATRA-resistant acute promyelocytic leukemia cells: P.N. Meyer, et al.; Leuk. Res. 32, 143 (2008) 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
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
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 |
| | | | | RELATED PRODUCT GROUPS | Stress & Heat Shock Proteins > Heat Shock Proteins [HSPs] / Chaperones / Related Products > HSP90 / HtpG / Related Products / Signal Transduction > Kinases / Related Products > Tyrosine Kinases / Related Products > Tyrosine Kinase Inhibitors / Natural Products / Antibiotics > Antibiotics > Antibiotics - Signal Transduction Pathway Modulators > Antibiotics - Other Signal Transduction Pathway Modulators / Natural Products / Antibiotics > Antibiotics > Antibiotics - Apoptosis Inducers & Inhibitors / Cancer > Antitumor Reagents > Antitumor Agents (Enzyme Inhibitors) | | | | | |
