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Merck
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Key Documents

EPS003

Sigma-Aldrich

CUDC 101

A potent inhibitor of HDACs and receptor tyrosine kinases

别名:

7-[[4-(3-Ethynylphenylamino)-7-methoxyquinazolin-6-yl]oxy]-N-hydroxyheptanamide, Heptanamide, 7-[[4-[(3-ethynylphenyl)amino]-7-methoxy-6-quinazolinyl]oxy]-N-hydroxy

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About This Item

经验公式(希尔记法):
C24H26N4O4
分子量:
434.49
分類程式碼代碼:
12352200
NACRES:
NA.41

化驗

≥98% (HPLC)

顏色

white

溶解度

DMSO: soluble

儲存溫度

−20°C

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 密鑰

PLIVFNIUGLLCEK-UHFFFAOYSA-N

相关类别

一般說明

A potent multitargeted inhibitor of histone deacetylase (HDAC) and the receptor kinases epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2), with IC50 values of 4.4, 2.4, and 15.7 nM, respectively.

Displays potent antiproliferative and proapoptotic activities against cultured and implanted tumor cells that are sensitive or resistant to several approved single-targeted drugs.

儲存類別代碼

10 - Combustible liquids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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Cheng-Jung Lai et al.
Cancer research, 70(9), 3647-3656 (2010-04-15)
Receptor tyrosine kinase inhibitors have recently become important therapeutics for a variety of cancers. However, due to the heterogeneous and dynamic nature of tumors, the effectiveness of these agents is often hindered by poor response rates and acquired drug resistance.
Xiong Cai et al.
Journal of medicinal chemistry, 53(5), 2000-2009 (2010-02-11)
By incorporating histone deacetylase (HDAC) inhibitory functionality into the pharmacophore of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) inhibitors, we synthesized a novel series of compounds with potent, multiacting HDAC, EGFR, and HER2
Ni Sima et al.
Translational oncology, 11(4), 1053-1064 (2018-07-10)
Drug resistance to chemotherapy occurs in many ovarian cancer patients resulting in failure of treatment. Exploration of drug resistance mechanisms and identification of new therapeutics that overcome the drug resistance can improve patient prognosis. Following a quantitative combination screen of

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