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AT13387

synthetic, orally bioavailable and small-molecule Hsp90 inhibitor

AT13387

Catalog No. A4056
Size Price Stock Qty
5mg $170.00 In stock
10mg $230.00 In stock
50mg $650.00 In stock
100mg $960.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

AT13387

Biological Activity

Description AT13387 is a synthetic, orally bioavailable and small-molecule inhibitor of heat shock protein 90 (Hsp90) with IC50 value of 18 nM in A375 cells.
Targets Hsp90          
IC50 18 nM (in A375 cells)          

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Chemical Properties

Cas No. 912999-49-6 SDF Download SDF
Chemical Name (2,4-dihydroxy-5-propan-2-ylphenyl)-[5-[(4-methylpiperazin-1-yl)methyl]-1,3-dihydroisoindol-2-yl]methanone
Canonical SMILES CC(C)C1=C(C=C(C(=C1)C(=O)N2CC3=C(C2)C=C(C=C3)CN4CCN(CC4)C)O)O
Formula C24H31N3O3 M.Wt 409.5
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition: Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

AT13387, discovered by a high-throughput x-ray craystallography fragment-based platform, is a non-geldanamycin heat shock proterin 90 (HPS90), a molecule chaperone regulating signal transduction pathways for cell growth and survival, inhibitor reportedly resulting in client protein degradation, suppression of signaling, and inducing cell cycle arrest and apoptosis. Since structurally unrelated to geldanamycin, it has high affinity for binding HSP90 (Kd = 0.5nM) and exhibited an in vitro cytotoxicity showing a median EC50 value of 41 nM. A long tumor-specific retention was observed in AT13387 during xenograft  studies, which indicated the possibility of less frequent dosing. However, preliminary results showed that the antitumor activity of AT13387 against solid tumor and leukemia models is similar to alvespimycin.

Reference

Min H. Kang, C. Patrick Reynolds, Peter J. Houghton, Denise Alexander, Christopher L. Morton, E. Anders Kolb, Richard Gorlick, Stephen T. Keir, Hernan Carol, Richard Lock, John M. Maris, Amy Wozniak, and Malcolm A. Smith. Initial Testing (Stage 1) of AT13387, an HSP90 Inhibitor, by the Pediatric Preclinical Testing Program. Pediatr Blood Cancer. 2012; 59(1): 185-188