17-AAG (17-allylamino-17-demethoxygeldanamycin, Telatinib, Tanespimycin, NSC-330507, CNF-101, KOS-953, GLD-36, CP 127374)

Semi-synthetic derivative of geldanamycin, demonstrating greater stability and lower in vivo toxicity than its parent compound. 17-AAG binds specifically to heat shock protein Hsp90 in a manner similar to geldanamycin, but the binding is weaker. \n\nSolubility: \nSoluble in DMSO at 150mg/ml; soluble in ethanol at 5mg/ml; very poorly soluble in water; maximum solubility in plain water is estimated to be about 20-50uM; buffers, serum, or other additives may increase or decrease the aqueous solubility.\n\nStorage and Stability:\nMay be stored at RT for short-term only. Long-term storage is recommended at -20 degrees C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.

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SPECIFICATIONS

Catalog Number

A0001-85

Size

250mg

Form

Supplied as a purple powder.

Purity

~99%

References

1. Schulte, T.W. and Neckers, L.M. \"The benzoquinone ansamycin 17-allylamino-17-demethoxygeldanamycin binds to HSP90 and shares important biologic activities with geldanamycin.\" Cancer Chemother. Pharmacol. 42:273-279 (1998). 2. Basso, A.D., et al. \"Ansamycin antibiotics inhibit Akt activation and cyclin D expression in breast cancer cells that overexpress HER2.\" Oncogene 21:1159-1166 (2002). 3. Kamal, A., et al. \"A high-affinity conformation of Hsp90 confers tumour selectivity on Hsp90 inhibitors.\" Nature 425:407-10 (2003). 4. Nguyen, D.M., et al. \"Sequence-dependent enhancement of paclitaxel toxicity in non-small cell lung cancer by 17-allylamino 17-demethoxygeldanamycin.\" J. Thorac. Cardiovasc. Surg. 118:908-915 (1999) 5. Solit, D.B., et al. \"Inhibition of heat shock protein 90 function down-regulates Akt kinase and sensitizes tumors to Taxol.\" Cancer Res. 63:2139-2144 (2003). 6. Vasilevskaya, I.A., et al. \"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.\" Mol Pharmacol. 65:235-243 (2004). 7. Kaur, G, et al. \"Antiangiogenic properties of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin: an orally bioavailable heat shock protein 90 modulator.\" Clin. Cancer Res. 10:4813-4821 (2004).