A multi-target inhibitor of HDACs, EGFR, and HER2
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CUDC-101

Item No. 16426

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
7-[[4-[(3-ethynylphenyl)amino]-7-methoxy-6-quinazolinyl]oxy]-N-hydroxy-heptanamide
CAS Number
1012054-59-9
Molecular Formula
C24H26N4O4
Formula Weight
434.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMF:PBS (pH 7.2) (1:9): 0.1 mg/mlDMSO: 2 mg/ml
λmax
225, 247, 334 nm
SMILES
COC1=CC2=C(C(NC3=CC=CC(C#C)=C3)=NC=N2)C=C1OCCCCCCC(NO)=O
InChi Code
InChI=1S/C24H26N4O4/c1-3-17-9-8-10-18(13-17)27-24-19-14-22(21(31-2)15-20(19)25-16-26-24)32-12-7-5-4-6-11-23(29)28-30/h1,8-10,13-16,30H,4-7,11-12H2,2H3,(H,28,29)(H,25,26,27)
InChi Key
PLIVFNIUGLLCEK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    10 mg

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    25 mg

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    Product Description

    CUDC-101 is a multi-target inhibitor, combining functional groups of potent inhibitors of human epidermal growth factor receptor (HER) kinases and histone deacetylases (HDACs). It potently blocks the receptor tyrosine kinases EGFR (aka HER1) and HER2 (IC50s = 2.4 and 16.4 nM, respectively).1 CUDC-101 also inhibits the activity of class I and class II HDACs at nanomolar concentrations (e.g., IC50s = 4.5, 12.6, 13.2, and 11.4 nM for HDAC1, 2, 4, and 5, respectively).1 It has only weak effects on over 60 other kinases when tested at 5 µM.1 CUDC-101 prevents the growth of a wide range of cancer cell lines in vitro, and slows tumor growth or induces tumor regression through cancer cell apoptosis in xenograft models.1 In cancer cells that have acquired resistance to single-target EGFR inhibitors, CUDC-101 blocks proliferation and reduces cell migration.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lai, C.J., Bao, R., Tao, W., et al. CUDC-101, a multitargeted inhibitor of histone deacetylase, epidermal growth factor receptor, and human epidermal growth factor receptor 2, exerts potent anticancer activity. Cancer Res. 70(9), 3647-3656 (2010).

    2. Wang, J., Pursell, N.W., Samson, M.E.S., et al. Potential advantages of CUDC-101, a multitargeted HDAC, EGFR, and HER2 inhibitor, in treating drug resistance and preventing cancer cell migration and invasion. Mol. Cancer Ther. 12(6), 925-936 (2013).