An Hsp90 inhibitor
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CUDC-305

Item No. 24683

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-amino-2-[[6-(dimethylamino)-1,3-benzodioxol-5-yl]thio]-N-(2,2-dimethylpropyl)-1H-imidazo[4,5-c]pyridine-1-ethanamine
CAS Number
1061318-81-7
Molecular Formula
C22H30N6O2S
Formula Weight
442.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 5 mg/mlEthanol: 5 mg/ml
λmax
208, 291 nm
SMILES
CN(C)C(C=C(OCO1)C1=C2)=C2SC3=NC4=C(N)N=CC=C4N3CCNCC(C)(C)C
InChi Code
InChI=1S/C22H30N6O2S/c1-22(2,3)12-24-8-9-28-14-6-7-25-20(23)19(14)26-21(28)31-18-11-17-16(29-13-30-17)10-15(18)27(4)5/h6-7,10-11,24H,8-9,12-13H2,1-5H3,(H2,23,25)
InChi Key
RVJIQAYFTOPTKK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    CUDC-305 is an orally bioavailable inhibitor of heat shock protein 90 (Hsp90; Item Nos. 22734 | 22735).1 It binds to Hsp90α and Hsp90β (IC50s = 100 and 103 nM for purified protein, respectively) as well as Hsp90 isolated from non-small cell lung cancer (NSCLC) cells resistant to erlotinib (Item No. 10483; IC50 = 70 nM).1,2 CUDC-305 induces degradation of Hsp90 client proteins in BT-474 breast cancer cells and inhibits proliferation of 40 human cancer cell lines (IC50s = 0.04-0.9 µM).1 It also reduces the levels of several oncoproteins including Akt and phosphorylated Akt, and ERK1/2 and phosphorylated ERK1/2 in a variety of cancer cell lines. CUDC-305 (40-160 mg/kg) dose-dependently reduces tumor growth in a U87MG glioblastoma mouse xenograft model and, when administered at a dose of 160 mg/kg, prolongs survival in a U87MG mouse orthotopic model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bao, R., Lai, C.-J., Qu, H., et al. CUDC-305, a novel synthetic HSP90 inhibitor with unique pharmacologic properties for cancer therapy. Clin Cancer Res. 15(12), 4046-4057 (2009).

    2. Bao, R., Lai, C.-J., Wang, D.-G., et al. Targeting heat shock protein 90 with CUDC-305 overcomes erlotinib resistance in non-small cell lung cancer. Mol. Cancer Ther. 8(12), 3296-3306 (2009).