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Sorafenib tosylate

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CAS:284461-73-0
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CAS:284461-73-0
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Products Intro: Product Name:Sorafenib tosylate
CAS:284461-73-0
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Lastest Price from Sorafenib tosylate manufacturers

  • Sorafinib
  • US $10.00 / KG
  • 2018-09-26
  • CAS:284461-73-0
  • Min. Order: 10G
  • Purity: 99%
  • Supply Ability: 10MT
  • Sorafenib tosylate
  • US $100.00 / KG
  • 2018-07-27
  • CAS:284461-73-0
  • Min. Order: 1KG
  • Purity: 99%
  • Supply Ability: Customized
Sorafenib tosylate Basic information
Overview Indications Mechanism of action Side effects References
Product Name:Sorafenib tosylate
Synonyms:Sorafenib free base for research;Sorafenib Free Base;Forafenib;Sorafenib free base(Bay43-9006);nexavar,sorafenib;Nexavar;Sorafenib-d4;2-PyridinecarboxaMide,4-[4-[[[[4-chloro-3-(trifluoroMethyl)phenyl]aMino]carbonyl]aMino]phenoxy]-N-Methyl-
CAS:284461-73-0
MF:C21H16ClF3N4O3
MW:464.83
EINECS:1308068-626-2
Product Categories:anti-neoplastic;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;Pharmaceutical intermediate;Amines;Inhibitor;Bay 43-9006;Sorafinib;Molecular Targeted Antineoplastic;All Inhibitors
Mol File:284461-73-0.mol
Sorafenib tosylate Structure
Sorafenib tosylate Chemical Properties
Melting point 202-204°C
storage temp. -20°C Freezer
CAS DataBase Reference284461-73-0(CAS DataBase Reference)
Safety Information
Risk Statements 68/20/21/22-37/38
Safety Statements 36-37-39
MSDS Information
Sorafenib tosylate Usage And Synthesis
OverviewSorafenib tosylate is the tosylate form of sorafenib, which is a drug approved for the treatment of hepatocellular carcinoma and the treatment of advanced renal cell carcinoma (primary kidney cancer). Hepatocellular carcinoma accounts for the vast majority of primary liver cancers (85–90%). [1] Approximately 70–90% of all hepatocellular cancer cases occur in patients with chronic liver disease and cirrhosis, with the main causes of cirrhosis including hepatitis B, hepatitis C and alcoholic liver disease.[1] Sorafenib is an oral receptor tyrosine kinase inhibitor that inhibits Raf serine/threonine kinases and receptor tyrosine kinases (vascular endothelial growth factor receptors 1, 2, 3 and platelet-derived growth factor-b, Flt-3 and c-kit) that are implicated in tumorigenesis and tumor progression.

Figure 1 the chemical structure of sorafenib;
IndicationsIt is indicated for the treatment of hepatocellular carcinoma and the treatment of advanced renal cell carcinoma (primary kidney cancer).
Mechanism of actionThe bi-aryl urea sorafenib is an oral multikinase inhibitor that inhibits both cell surface tyrosine kinase receptors and downstream intracellular serine/threonine kinases in the Ras/MAPK cascade.[2-4] Receptor tyrosine kinases inhibited by sorafenib include vascular endothelial growth factor receptor (VEGFR)-1, VEGFR-2, VEGFR-3, platelet-derived growth factor receptor (PDGFR)-b, c-KIT, FMS-like tyrosine kinase 3 (FLT-3) and RET. Intracellular Raf serine/threonine kinase isoforms inhibited by sorafenib include Raf-1 (or C-Raf), wild-type B-Raf and mutant B-Raf.[3, 4] These kinases are involved in tumour cell proliferation and tumour angiogenesis.[3, 4]
The antiproliferative activity of sorafenib is variable in different tumor types and largely depends on the oncogenic signaling pathways that mediate tumor proliferation. Sorafenib has also been shown to induce apoptosis in several tumor cell lines. Although the mechanism through which sorafenib induces apoptosis is not fully elucidated and may vary between cell lines, a commonly observed theme is the inhibition of phosphorylation of the initiation factor eIF4E and loss of the antiapoptotic protein myeloid cell leukemia-1 (MCL-1)[5]. Recently, sorafenib was shown to inhibit hepatitis C viral replication in vitro[6], and in vitro studies have also shown some direct effects on immune cells [7]. Whether these effects
Side effectsThe most common adverse reactions (20%), considered to be related to sorafenib, in patients with HCC or RCC are fatigue, weight loss, rash/desquamation, hand-foot skin reaction, alopecia, diarrhea, anorexia, nausea and abdominal pain [12].
Across all tumor types, common side effects (> 10%) include hypertension (9 -- 13%, grade 4: < 1%; onset: ~ 3 weeks), fatigue (37 -- 46%), sensory neuropathy (13%), pain (11%), rash/desquamation (19 -- 40%; grade 3: 1%), handfoot syndrome (21 -- 30%; grade 3: 6 -- 8%), alopecia (14 -- 27%), pruritis (14 -- 19%), dry skin (10 -- 11%), hypoalbuminemia (59%), hypophosphatemia (35 -- 45%; grade 3: 11 -- 13%; grade 4: < 1%), diarrhea (43 -- 55%; grade 3: 2 -- 10%; grade 4: < 1%), lipase increased (40 -- 41%, usually transient), amylase increased (30 -- 34, usually transient), abdominal pain (11 -- 31%), weight loss (10 -- 30%), anorexia (16 -- 29%), nausea (23 -- 24%), vomiting (15 -- 16%), constipation (14 -- 15%), muscle pain, weakness, dyspnea (14%), cough (13%) and hemorrhage (15 -- 18%; grade 3: 2 -- 3%; grade 4: 2%). Laboratory abnormalities attributable to sorafenib use are also seen and include lymphopenia (23 -- 47%; grades 3/4: 13%), thrombocytopenia (12 -- 46%; grades 3/4: 1 -- 4%), international normalized ration (INR) increased (42%), neutropenia (18%; grades 3/4: 5%), leucopenia, liver dysfunction (11%; grade 3: 2%; grade 4: 1%).
Less frequent side effects (> 1 -- 10) include cardiac ischemia/infarction (3%), flushing, headache (10%), depression, fever, acne, exfoliative dermatitis, decreased appetite, dyspepsia, dysphagia, esophageal varices bleeding (2%), glossodynia, mucositis, stomatitis, xerostomia, erectile dysfunction, anemia, transaminases increased (transient), joint pain (10%), arthralgia, myalgia, hoarseness and flu-like syndrome.
Rare (< 1%) side effects of sorafenib include acute renal failure, alkaline phosphatase increased, arrhythmia, bilirubin increased, bone pain, cardiac failure, cerebral hemorrhage, congestive heart failure, dehydration, eczema, epistaxis, erythema multiforme, folliculitis, gastritis, gastrointestinal hemorrhage, gastrointestinal perforation, gastrointestinal reflux, gynecomastia, hypersensitivity (skin reaction, urticaria), hypertensive crisis, hyponatremia, hypothyroidism, infection, jaundice, myocardial infarction (MI), mouth pain, myocardial ischemia, pancreatitis, pleural effusion, preeclampsialike syndrome (reversible hypertension and proteinuria), renal failure, respiratory hemorrhage, reversible posterior leukoencephalopathy syndrome (RPLS), rhinorrhea, skin cancer (squamous cell/keratoacanthomas), thromboembolism, tinnitus, transient ischemic attack, tumor lysis syndrome, tumor pain and voice alteration.
References
  1. El-Serag HB, Rudolph KL. Hepatocellular carcinoma: epidemiology and molecular carcinogenesis. Gastroenterology 2007 Jun; 132 (7): 2557-76
  2. Adnane L, Trail PA, Taylor I, et al. Sorafenib (BAY 43- 9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature. Methods Enzymol 2005; 407: 597-612
  3. Wilhelm S, Carter C, Lynch M, et al. Discovery and development of sorafenib: a multikinase inhibitor for treating cancer. Nat Rev Drug Discov 2006 Oct; 5 (10): 835-44
  4. Wilhelm SM, Carter C, Tang LY, et al. BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis. Cancer Res 2004 Oct 1; 64 (19): 7099-109
  5. Yu C, Bruzek LM, Meng XW, et al. The role of Mcl-1 downregulation in the proapoptotic activity of the multikinase inhibitor BAY 43-9006. Oncogene 2005;24:6861-9
  6. Himmelsbach K, Sauter D, Baumert TF, et al. New aspects of an anti-tumour drug: sorafenib efficiently inhibits HCV replication. Gut 2009;58:1644-53
  7. Molhoek KR, McSkimming CC, Olson WC, et al. Apoptosis of CD4(+) CD25(high) T cells in response to Sirolimus requires activation of T cell receptor and is modulated by IL-2. Cancer Immunol Immunother 2009;58:867-76
  8. Strumberg D, Richly H, Hilger RA, et al. Phase I clinical and pharmacokinetic study of the Novel Raf kinase and vascular endothelial growth factor receptor inhibitor BAY 43-9006 in patients with advanced refractory solid tumors. J Clin Oncol 2005;23:965-72
  9. Clinical Pharmacology and Biopharmaceutics NDA Review for Sorafenib Tosylate (NDA 21 923), F.C.F.D.E.A. RESEARCH, Editor, 2005
  10. BAY 43-9006 (sorafenib) Investigator’s Brochure. Bayer Healthcare AG,Version 10.0, July 1, 2009
  11. European Medicines Agency. Sorafenib (Nexavar): summary of product characteristics [online].
  12. Blanchet B, Billemont B, Barete S, et al. Toxicity of sorafenib: clinical and molecular aspects. Expert Opin Drug Saf 2010;9:275-87
  13. https://www.drugs.com/cdi/sorafenib.html
Chemical PropertiesLight Yellow Solid
UsesA potent RAF kinase inhibitor. Antineoplastic
UsesMultiple kinase inhibitor targeting both RAF kinase and receptor tyrosine kinases that promote angiogensis. Antineoplastic.
UsesSorafenib 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.
UsesSorafenib Tosylate (Bay 43-9006) is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively - See more at: http://www.selleckchem.com/products/Sorafenib-Tosylate.html#sthash.BjHEmCf3.dpuf
Brand nameNexavar (Bayer HealthCare); Xarelto (Bayer HealthCare).
Sorafenib tosylate Preparation Products And Raw materials
Tag:Sorafenib tosylate(284461-73-0) Related Product Information
4-Methoxyphenylacetone Formamide,Deionized SORAFENIB N-OXIDE Vatalanib base Methyl Methyl acrylate N,N-Dimethylformamide Trifluoromethyl Diphenyldiethoxysilane Basic Violet 1 Pirfenidone Difluorochloromethane Acetonitrile Benzamide PHENYL VALERATE CHLOANTRANILIPROLE Methylparaben Methanol