1012054-59-9 Usage
Description
CUDC-101 (1012054-59-9) is a novel hybrid dual-acting HDAC and receptor tyrosine kinase inhibitor. It is a potent HDAC inhibitor which also inhibits EGFR and HER2,? IC50?= 4.4, 2.4 and 15.7 nM respectively.1?It not only blocks EGFR and HER2 but also attenuates multiple compensatory pathways such as AKT, HER3 and MET which enable tumor cells to escape the effects of conventional EGFR/HER2 inhibitors.1,2
Uses
Different sources of media describe the Uses of 1012054-59-9 differently. You can refer to the following data:
1. Inhibitor of HDAC, EGFR, and HER2 with an IC50 of 4.4, 2.4, and 15.7 nM, respectively.
2. CUDC-101 is a potent multi-acting HDAC (histone deacetylase), EGFR (epidermal growth factor receptor), and HER2 ( human epidermal growth factor receptor 2) inhibitor for the treatment of cancer.
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.
References
1) Lai?et al. (2010),?CUDC-101, a multitargeted inhibitor of histone deacetylase, epidermal growth factor receptor, and human epidermal growth factor receptor 2, exerts potential anticancer activity; Cancer Res.,?70?3647
2) Cai?et al.?(2010), Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer; J. Med. Chem.,?53?2000
Check Digit Verification of cas no
The CAS Registry Mumber 1012054-59-9 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,0,1,2,0,5 and 4 respectively; the second part has 2 digits, 5 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 1012054-59:
(9*1)+(8*0)+(7*1)+(6*2)+(5*0)+(4*5)+(3*4)+(2*5)+(1*9)=79
79 % 10 = 9
So 1012054-59-9 is a valid CAS Registry Number.
1012054-59-9Relevant articles and documents
Discovery of 7-(4-(3-Ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N- hydroxyheptanamide (CUDC-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer
Cai, Xiong,Zhai, Hai-Xiao,Wang, Jing,Forrester, Jeffrey,Qu, Hui,Yin, Ling,Lai, Cheng-Jung,Bao, Rudi,Qian, Changgeng
supporting information; experimental part, p. 2000 - 2009 (2010/07/17)
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 inhibition and identified 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N- hydroxyheptanamide 8 (CUDC-101) as a drug candidate, which is now in clinical development. 8 displays potent in vitro inhibitory activity against HDAC, EGFR, and HER2 with an IC50 of 4.4, 2.4, and 15.7 nM, respectively. In most tumor cell lines tested, 8 exhibits efficient antiproliferative activity with greater potency than vorinostat (SAHA), erlotinib, lapatinib, and combinations of vorinostat/erlotinib and vorinostat/lapatinib. In vivo, 8 promotes tumor regression or inhibition in various cancer xenograft models including nonsmall cell lung cancer (NSCLC), liver, breast, head and neck, colon, and pancreatic cancers. These results suggest that a single compound that simultaneously inhibits HDAC, EGFR, and HER2 may offer greater therapeutic benefits in cancer over single-acting agents through the interference with multiple pathways and potential synergy among HDAC and EGFR/HER2 inhibitors.
TARTRATE SALTS OF QUINAZOLINE BASED EGFR INHIBITORS CONTAINING A ZINC BINDING MOIETY
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Page/Page column 68, (2009/04/24)
The present invention relates to tartrate salts of quinazoline containing zinc-binding moiety based derivatives that are inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and their use in the treatment of EGFR-TK related diseases and disorders such as cancer. The tartrate salts may further act as HDAC inhibitors.
