|
| CUDC-101 Basic information |
Product Name: | CUDC-101 | Synonyms: | CUDC101;CUDC-101;7-[[4-(3-Ethynylphenylamino)-7-methoxyquinazolin-6-yl]oxy]-N-hydroxyheptanamide;CUDC101; CUDC 101; CUDC-101.;CS-330;CUDC101;CUDC 101;HeptanaMide, 7-[[4-[(3-ethynylphenyl)aMino]-7-Methoxy-6-quinazolinyl]oxy]-N-hydroxy-;7-[[4-[(3-Ethynylphenyl)aMino]-7-Methoxy-6-quinazolinyl]oxy]-N-hydroxyheptanaMide | CAS: | 1012054-59-9 | MF: | C24H26N4O4 | MW: | 434.49 | EINECS: | | Product Categories: | Inhibitor;Antineoplastic;Inhibitors | Mol File: | 1012054-59-9.mol | |
| CUDC-101 Chemical Properties |
Melting point | 174-177℃ | density | 1.28 | storage temp. | -20°C | solubility | DMSO: soluble | form | solid | pka | 9.47±0.20(Predicted) | color | White or off-white | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. | InChIKey | PLIVFNIUGLLCEK-UHFFFAOYSA-N |
| CUDC-101 Usage And Synthesis |
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 | Inhibitor of HDAC, EGFR, and HER2 with an IC50 of 4.4, 2.4, and 15.7 nM, respectively. | Uses | 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. | target | EGFR | 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 |
| CUDC-101 Preparation Products And Raw materials |
|