An Hsp90 inhibitor
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PU-H71 (hydrate)

Item No. 11450

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-amino-8-[(6-iodo-1,3-benzodioxol-5-yl)thio]-N-(1-methylethyl)-9H-purine-9-propanamine, hydrate
CAS Number
1202865-65-3
Molecular Formula
C18H21IN6O2S • XH2O
Formula Weight
512.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 12 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 10 mg/ml
λmax
219, 285, 349 nm
SMILES
CC(C)NCCCN1C2=NC=NC(N)=C2N=C1SC3=C(I)C=C4C(OCO4)=C3.O
InChi Code
InChI=1S/C18H21IN6O2S.H2O/c1-10(2)21-4-3-5-25-17-15(16(20)22-8-23-17)24-18(25)28-14-7-13-12(6-11(14)19)26-9-27-13;/h6-8,10,21H,3-5,9H2,1-2H3,(H2,20,22,23);1H2
InChi Key
ZUGBRIZOLBTCHT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    1 mg

    $109

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    5 mg

    $409

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    10 mg

    $763

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    Cayman Chemical
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    Product Description

    PU-H71 is an inhibitor of heat shock protein 90 (Hsp90; IC50 = 16.1 nM in a fluorescence polarization assay).1 It induces HER2 degradation via disrupting Hsp90-HER2 interactions and decreases growth in SK-BR-3 breast cancer cells (IC50 = 50 nM for both). PU-H71 (1 µM) decreases viability of MM.1S and dexamethasone-resistant MM.1R multiple myeloma cells. It induces cell cycle arrest at the G1/S phase in MM.1R cells when used at a concentration of 100 nM.2 PU-H71 (75 mg/kg every other day) decreases tumor volume in MDA-MB-231 and HCC1806 breast cancer xenograft mouse models.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. He, H., Zatorska, D., Kim, J., et al. Identification of potent water soluble purine-scaffold inhibitors of the heat shock protein 90. J. Med. Chem. 49(1), 381-390 (2006).

    2. Usmani, S.Z., Bona, R.D., Chiosis, G., et al. The anti-myeloma activity of a novel purine scaffold HSP90 inhibitor PU-H71 is via inhibition of both HSP90A and HSP90B1. J. Hematol. Oncol. 3(40), 1-8 (2010).

    3. Caldas-Lopes, E., Cerchietti, L., Ahn, J.H., et al. Hsp90 inhibitor PU-H71, a multimodal inhibitor of malignancy, induces complete responses in triple-negative breast cancer models. Proc. Natl. Acad. Sci. USA 106(20), 8368-8373 (2009).