Regorafenib
Cat. No.:YN350029
CAS No. :755037-03-7
产品名称: | Regorafenib |
CAS No.: | 755037-03-7 |
Chemical Name: | 4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide |
Synonyms: | 瑞戈非尼; BAY 73-4506 |
分子量: | 482.82 |
分子式: | C₂₁H₁₅ClF₄N₄O₃ |
SMILES: | O=C(NC1=CC=C(C(C(F)(F)F)=C1)Cl)NC2=CC=C(OC3=CC(C(NC)=O)=NC=C3)C=C2F |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | Regorafenib (BAY 73-4506) 是一种多靶点受体酪氨酸激酶抑制剂,抑制VEGFR1/2/3,PDGFRβ,Kit,RET和Raf-1的IC50分别为13/4.2/46,22,7,1.5 和2.5 nM。 |
IC50和靶点: | [{name:"Raf-1:2.5 nM (IC50)"},{name: "Tie2:311 ± 46 nM (IC50)"},{name: "VEGFR2:4.2 nM (IC50)"},{name: "VEGFR1:13 nM (IC50)"},{name: "BRafV600E:19 nM (IC50)"},{name: "PDGFRβ:22 nM (IC50)"},{name: "Braf:28 nM (IC50)"},{name: "VEGFR3:46 nM (IC50)"}] |
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Wilhelm, S.M., Dumas, J., Adnane, L., et al.Regorafenib (BAY 73-4506): A new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activityInt. J. Cancer129(1),245-255(2011)
Uitdehaag, J.C.M., de Roos, J.A.D.M., van Doornmalen, A.M., et al.Comparison of the cancer gene targeting and biochemical selectivities of all targeted kinase inhibitors approved for clinical usePLoS One9(3),1-13(2014)
Ravi, S., and Singal, A.K.Regorafenib: An evidence-based review of its potential in patients with advanced liver cancerCore Evid.9,81-87(2014)