AT13387
Catalog #
27736-2
$275
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Description
AT13387, discovered by a high-throughput x-ray craystallography fragment-based platform, is a non-geldanamycin inhibitor of heat shock proterin 90 (HPS90), a molecule chaperone regulating signal transduction pathways for cell growth and survival. It has high affinity for binding HSP90 (Kd = 0.5nM) and exhibited an in vitro cytotoxicity showing a median EC50 value of 41 nM. The antitumor activity of AT13387 against solid tumor and leukemia models is similar to alvespimycin.
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Synonyms
(2,4-dihydroxy-5-propan-2-ylphenyl)-[5-[(4-methylpiperazin-1-yl)methyl]-1,3-dihydroisoindol-2-yl]methanone
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Product Data Gallery
Product Info
Storage and Usage
Citations
Target(s)
HSP90
Formula
C24H31N3O3
MW
409.5 Da
Solubility
Soluble in DMSO
Biological Activity
AT13387 is a potent inhibitor of the proliferat ion and survival of many different cell lines (such as MES-SA cell line) from a variety of different tumor types. Across a panel of 30 tumor cell lines, AT13387 potently inhibits cell proliferation with GI50 values in the range 13-260 nM. AT13387 inhibits proliferation of the non-tumorigenic human prostate epithelial cell line PNT2 with a GI50 value of 480 nM. The inhibition of a number of isolated kinases by AT13387 is also investigated including CDK 1, CDK 2, CDK4, FGFR3, PKB-b, JAK2, VEGFR2, PDGFRβ and Aurora B. None of the tested kinases are significantly inhibited at concentrations below 30 µM.
CAS Registry #
912999-49-6
References
Min H. et al. Pediatr Blood Cancer. 2012; 59(1): 185-188.
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