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Merck

EPS003

CUDC 101

A potent inhibitor of HDACs and receptor tyrosine kinases

동의어(들):

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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제품정보 (DICE 배송 시 비용 별도)

실험식(Hill 표기법):
C24H26N4O4
CAS 번호:
Molecular Weight:
434.49
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.41
Assay:
≥98% (HPLC)
Quality level:
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Quality Level

assay

≥98% (HPLC)

color

white

solubility

DMSO: soluble

storage temp.

−20°C

SMILES string

N(O)C(=O)CCCCCCOc1cc2c(ncnc2Nc3cc(ccc3)C#C)cc1OC

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

General description

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.


저장 등급

10 - Combustible liquids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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시험 성적서(COA)

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문서 라이브러리 방문



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