CUDC-101, Free Base **

产品名称：CUDC-101, Free Base
产品货号：LC  C-8460
产品规格：10 MG
CUDC-101 is a potent 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.  It inhibted EGFR and Her2 phosphorylation, reduced cell proliferation and induced apoptosis in HCC827 non-small cell lung cancer (NSCLC) xenografts.  CUDC-101 inhibited EGFR and induced upregulation of acetylated histone H3 in a dose-dependent fashion.  CUDC-101 is efficacious in EGFR inhibitor sensitive and resistant NSCLC cell lines and xenografts.  CUDC-101 is also efficacious in epidermoid, pancreatic, and hepatocellular cancer cell lines and xenografts.  Bao, R., et al.  "Potent Anti-Cancer Activity In Vitro and In Vivo by a Novel, Small Molecule Inhibitor of HDAC, EGFR and Her2."  CUDC-101 inhibted histone deacetylase and synergistically blocked key regulators of EGFR/HER2 signaling pathways.  It also attenuated multiple compensatory pathways including AKT, HER3, and MET, which enable cancer cells to escape the effects of conventional EGFR/HER2 inhibitors.  CUDC-101 might improve the treatment of tumors that cannot be controlled with single-target agents.  Lai, C.J., et al.  "CUDC-101, a multitargeted inhibitor of histone deacetylase, epidermal growth factor receptor, and human epidermal growth factor receptor 2, exerts potent anticancer activity."  Cancer Res. 70:  3647-3656 (2010).
CUDC-101 inhibited the proliferation of most tumor cell lines tested with greater potency than vorinostat (SAHA), erlotinib, lapatinib, and combinations of vorinostat/erlotinib and vorinostat/lapatinib.  In vivo, CUDC-101 promoted tumor regression in various cancer xenograft models such as non-small cell lung cancer (NSCLC), liver, breast, head and neck, colon, and pancreatic cancers.  Cai, X., et al.  "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:  2000-2009 (2010).
Our CUDC-101 product is the free base, whose CAS number is given above.  The CAS number of the hydrochloride salt is 1133147-76-8.
Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 28 mg/mL; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 20-50 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility.  Disposal:  A

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