EPS003
CUDC 101
A potent inhibitor of HDACs and receptor tyrosine kinases
Synonyme(s) :
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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A propos de cet article
Formule empirique (notation de Hill) :
C24H26N4O4
Numéro CAS:
Poids moléculaire :
434.49
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.41
Assay:
≥98% (HPLC)
Quality level:
Service technique
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Laissez-nous vous aiderQuality 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.
Displays potent antiproliferative and proapoptotic activities against cultured and implanted tumor cells that are sensitive or resistant to several approved single-targeted drugs.
Classe de stockage
10 - Combustible liquids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_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