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AT13387

Cat. No. M1949
AT13387 Structure
Size Price Availability Quantity
5mg USD 220 In stock
10mg USD 310 In stock
50mg USD 880 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

AT13387 is a non-geldanamycin inhibitor of HSP90, it inhibited the proliferation of imatinib-sensitive (GIST882, GIST-T1) and -resistant (GIST430, GIST48) cell lines, including those resistant to the geldanamycin analogue HSP90 inhibitor, 17-AAG. AT13387 showed a median EC(50) value of 41 nM and exhibited activity consistent with a cytotoxic effect in vitro. In vivo, antitumor activity of AT13387 was showed in both the imatinib-sensitive, GIST-PSW, xenograft model and a newly characterized imatinib-resistant, GIST430, xenograft model. AT13387 has shown activity against a wide array of tumor cell lines, including lung cancer cell lines. While AT13387 was rapidly cleared from blood, its retention in tumor xenografts was markedly extended, and it was efficacious in a range of xenograft models. A combination of AT13387 and imatinib treatment in the imatinib-resistant GIST430 model significantly enhanced tumor growth inhibition over either of the monotherapies.

Protocol
Cell Experiment
Cell lines HCT116, A549, MCF-7, U266, PANC1, Huh-7, DU145, MES-SA, SKOV3, HL60, A375 and TFK-1 cells line
Preparation method Proliferation assays.
Cells were seeded into 96-well plates before the addition of compound in 0.1% (v/v) DMSO. GI50 were determined using a 10-point dose response curve for three cell doubling times. After compound incubation 10% (v/v), Alamar blue (Biosource International, Camarillo, CA, USA) was added, and cells were incubated for a further 4 h. Fluorescence was read at λex = 535 nm and λem = 590 nm.
Concentrations 0~1 μ M
Incubation time 48 or 72 h
Animal Experiment
Animal models Athymic mice bearing NCI-H1975 xenografts
Formulation 17.5% (w/v) hydroxypropyl-β-cyclodextrin
Dosages 70 mg/kg on days 1, 4, 8, 12 and 16; 55 mg/kg on days 1, 4, 8, 12 and 16; or 90 mg/kg on days 1, 8 and 16.
Administration intraperitoneally
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 409.52
Formula C24H31N3O3
CAS Number 912999-49-6
Purity >99%
Solubility DMSO 25 mg/mL
Storage at -20°C
References

The HSP90 inhibitor, AT13387, is effective against imatinib-sensitive and -resistant gastrointestinal stromal tumor models.
Smyth T, et al. Mol Cancer Ther. 2012 Aug;11(8):1799-808. PMID: 22714264.

The heat shock protein 90 inhibitor, AT13387, displays a long duration of action in vitro and in vivo in non-small cell lung cancer.
Graham B, et al. Cancer Sci. 2012 Mar;103(3):522-7. PMID: 22181674.

Initial testing (Stage 1) of AT13387, an HSP90 inhibitor, by the pediatric preclinical testing program.
Kang MH, et al. Pediatr Blood Cancer. 2012 Jul 15;59(1):185-8. PMID: 21538821.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: AT13387 supplier, HSP90, inhibitors

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