284461-73-0 2-Pyridinecarboxamide,4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]phenoxy]-N-me CAS NO.284461-73-0

melting point 202-204°c
storage temp. -20°c freezer
cas database reference 284461-73-0(cas database reference)
safety information
msds information
sorafenib tosylate usage and synthesis
sorafenib tosylate sorafenib tosylate is a novel multi-targeted anticancer drug and was successfully developed by the german pharmaceutical company bayer and can simultaneously act on both the tumor cell and tumor vasculature. it has dual anti-tumor effects:
it not only directly inhibits the proliferation of tumor cells either by blocking the raf/mek/erk-mediated cell signaling pathway but also indirectly inhibit the growth of tumor cells through inhibiting vegf and platelet-derived growth factor (pdgf) receptor which blocks tumor angiogenesis.
it shows a wide range of anti-tumor activity in preclinical animal studies. in randomized clinical studies of patients with advanced kidney cancer phase iii in europe and the united states, 903 cases of patients of advanced kidney cancer who have received a systemic therapy (chemotherapy or immune) were randomly divided into two groups, one group received sorafenib tosylate (referred sorafenib), the other group received placebo. there were 222 cases of deaths occurring during the interim analysis. the result showed that objective efficacy of these two groups was 10% and 2%, respectively. moreover, there are 74% and 53% of the patients, respectively, with their tumor remaining stable.
the progression-free survival rate in sorafenib group has been extended twice compared with the placebo group (5.8vs2.8 months with a risk ratio of 0.51). also, compared with placebo, sorafenib can significantly improve the quality of life of patients. the survival period of the sorafenib group is longer than that of the placebo group with the risk ratio being 0.72, but this difference did not reach statistical significance, as this result is only the result of the interim analysis and therefore we need to wait for the final analysis to make the final comparison of the survival period.
the tolerance of the sorafenib treatment is excellent with the main side effects being controllable diarrhea, rash, fatigue, hand-foot syndrome, hypertension, hair loss, nauseaomiting and loss of appetite.
in december 2005, the us food and drug administration (fda) have approved it for marketing as the first-line drug for the treatment for advanced kidney cancer.
in october 2007, the european medicines evaluation agency (emea) has approved sorafenib (nexavar) for the treatment of hepatocellular carcinoma.
in november 2007, the us food and drug administration approved nexavar for the treatment of unresectable hepatocellular carcinoma.
in august 2009, approved by the chinese state food and drug administration, the sorafenib tosylate tablets (trade name: nexavar) of the german pharmaceutical bayer company bayer sorafenib tosylate tablets (trade name: nexavar) have officially entered into the chinese market for the treatment of inoperable advanced liver cancer patients.
the above information is edited by the chemicalbook of dai xiongfeng.
treatment for advanced liver cancer the incidence of liver cancer is approximately twenty hundred thousandths due to that the liver cancer early symptoms are not obvious with nearly 80% of patients diagnosed only at the advanced stage. half of the world's liver cancer patients are in china while among the primary factors of causing liver cancer in china, the hepatitis b is in the first row. this causative factor of liver cancer is quite different from the liver cancer in europe and the united states.
researchers from several countries has published a report on a new american "new england journal of medicine," and said that they selected 602 patients with advanced liver cancer in the united states, europe and australia and other countries for study. none of these patients have ever received systemic therapy. the results showed that compared with placebo, taking sorafenib (nexavar) allow overall survival with advanced hepatocellular carcinoma or primary liver cancer being increased by about 44% while delaying disease progression time by 73%.
one of the major person in charge of the study, jord• bruning fox from the clinical hospital of barcelona, ??spain said, because of the prevalence of hepatitis b and hepatitis c, the worldwide death toll of liver cancer is still rising. the new study has showed that nexavar as a new option for treating liver cancer can play a role of prolonging survival rate of the patients. this result is "encouraging."
nexavar is produced by bayer healthcare, which can act on both the tumor cell and tumor vasculature. in june of the last year, the researchers has introduced in the annual meeting of the american society of clinical oncology, said that they selected patients with advanced liver cancer in asia and the pacific for study and had found that nexavar can prolong the survival of these patients by about 47%. it is also the only one drug which had been proven to be able to significantly prolong overall survival in patients with advanced liver cancer drugs.
the drugs have been approved for the treatment of liver cancer in the united states and europe bayer healthcare in august 2009 has released a press and said, nexavar has been approved by china's state food and drug administration for the treatment of patients with advanced liver cancer which is inoperable.
uses sorafenib is a novel multi-targeted oral drug for treatment of tumors.
chemical properties light yellow solid
usage a potent raf kinase inhibitor. antineoplastic
usage multiple kinase inhibitor targeting both raf kinase and receptor tyrosine kinases that promote angiogensis. antineoplastic.
usage sorafenib tosylate (bay 43-9006, nexavar) is a small molecular inhibitor of vegfr, pdgfr, c-raf and b-raf with ic50s of 18 nm, 10 nm, 3 nm and 15 nm, respectively.