AT13387

AT13387

Catalog Number:
L002368979APE
Mfr. No.:
APE-A4056
Price:
$318
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      • Overview
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          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.

      • Properties
        • Alternative Name
          (2,4-dihydroxy-5-propan-2-ylphenyl)-[5-[(4-methylpiperazin-1-yl)methyl]-1,3-dihydroisoindol-2-yl]methanone
          CAS Number
          912999-49-6
          Molecular Formula
          C24H31N3O3
          Molecular Weight
          409.5
          Appearance
          A solid
          Purity
          98.00%
          Solubility
          insoluble in H2O; ≥13.25 mg/mL in DMSO; ≥47.7 mg/mL in EtOH with ultrasonic
          Storage
          Store at -20°C

          * For Research Use Only

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