A selective inhibitor of Hsp90
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Onalespib

Item No. 10655

Technical Information
Formal Name
[1,3-dihydro-5-[(4-methyl-1-piperazinyl)methyl]-2H-isoindol-2-yl][2,4-dihydroxy-5-(1-methylethyl)phenyl]-methanone
CAS Number
912999-49-6
Synonyms
  • AT-13387
Molecular Formula
C24H31N3O3
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:5): 0.16 mg/mlDMSO: 20 mg/mlEthanol: 10 mg/ml
λmax
259, 293 nm
SMILES
OC1=CC(O)=C(C(C)C)C=C1C(N2CC(C=CC(CN3CCN(C)CC3)=C4)=C4C2)=O
InChi Code
InChI=1S/C24H31N3O3/c1-16(2)20-11-21(23(29)12-22(20)28)24(30)27-14-18-5-4-17(10-19(18)15-27)13-26-8-6-25(3)7-9-26/h4-5,10-12,16,28-29H,6-9,13-15H2,1-3H3
InChi Key
IFRGXKKQHBVPCQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Onalespib is a selective inhibitor of Hsp90 (IC50 = 18 nM).1 It induces the degradation of specific Hsp90 client proteins, including mutant EGFR, for up to seven days in tumor cell lines in vitro and up to three days in vivo.1,2 Onalespib is retained in tumor xenografts and is efficacious in a range of xenograft models.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Woodhead, A.J., Angove, H., Carr, M.G., et alDiscovery of (2,4-dihydroxy-5-isopropylphenyl)-[5-(4-methylpiperazin-1-ylmethyl)-1,3-dihydroisoindol-2-yl]methanone (AT13387), a novel inhibitor of the molecular chaperone Hsp90 by fragment based drug design. J. Med. Chem. 53, 5956-5969 (2010).

    2. Graham, B., Curry, J., Smyth, T., et alThe heat shock protein 90 inhibitor, AT13387, displays a long duration of action in vitro and in vivo in non-small cell lung cancer. Cancer Sci. 103(3), 522-527 (2012).