Sorafenib CAS: 284461-73-0
MF: C21H16ClF3N4O3
MW: 464.82

Sorafenib (CAS 284461-73-0)

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Sorafenib is rated 5.0 out of 5 by 2.
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Alternativa namn: Sorafenib is also known as Sorafenibum.
Ansökan Sorafenib is an inhibitor of Raf-1 and B-RAF as well as several tyrosine kinases. Sorafenib also inhibits tumor angiogenesis by inducing tumor cell apopt
Momsregistreringsnummer :: 284461-73-0
Purity: ≥99%
Molecular Weight: 464.82
Molecular Formula: C21H16ClF3N4O3
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data (including water content).

Sorafenib is a RAF kinase inhibitor which suppresses ERK phosphorylation. Studies indicate that Sorafenib induces c-Raf phosphorylation at both Ser-43 and Ser-259. When combined with vitamin K1, phosphorylation is increased at these serine residues. Sorafenib also induces the phosphorylation of PKA. In addition, Sorafenib induces c-Met phosphorylation at Tyr-1349, which consequently induces PI3K-Akt phosphorylation. Studies determined that Sorafenib inhibits other kinases such as Flk-1 (VEGFR2), PDGFR (platelet-derived growth factor receptor), Flt-3/Flk-2 (FLT3), Ret, and c-Kit. Sorafenib is an inhibitor of Raf-1, Raf-B, PDGFR-βand Flt-4. Its ability to affect the Raf/Mek/Erk pathway makes it useful in cancer research studies. Sorafenib is also known as Sorafenibum, BAY 43-9006, and 4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]phenoxy]-N-methyl-2-pyridinecarboxamide.


Konferenser

1. Richly, H., et al. 2003. Int J Clin Pharmacol Ther. 41: 620-621. PMID: 14692720

2. Khire, U.R., et al. 2004. Bioorg. Med. Chem. Lett. 14: 783-786. PMID: 14741289

3. Wilhelm, S.M., et al. 2004. Cancer Res. 64: 7099-7109. PMID: 15466206

4. Liu, L., et al. 2006. Cancer Res. 66: 11851-11858. PMID: 17178882

5. Rini, B.I. 2006. Expert Opin Pharmacother. 7: 453-461. PMID: 16503817

6. Carr, B.I., et al. 2011. Cancer Biol Ther. [Epub ahead of print]. PMID: 21734462

Usage :
Sorafenib is soluble in organic solvents and sparingly soluble in aqueous buffers.
Physical State :
Solid
Solubility :
Soluble in DMSO (~20 mg/ml), methanol, DMF (~20 mg/ml), 1:2 solution of DMSO:PBS(PH 7.2 ) (~0.3 mg/ml), 100% ethanol (<1 mg/ml (mM)), ethyl acetate, and water (1 mg/ml (mM) at 25° C).
LAGRING :
Store at -20° C
Melting Point :
202-204° C
Refractive Index :
n20D 1.63 (Predicted)
IC50 :
Raf-1 : IC50 = 6 nM (cancer cells); B-Raf: IC50 = 22 nM (cancer cells); Vascular endothelial growth factor receptors 2 ascular endothelial growth factor receptors 2 : IC50 = 90 nM (cancer cells); Vascular endothelial growth factor receptors 2 ascular endothelial growth factor receptors 3 : IC50 = 15 nM (cancer cells); Platelet-derived growth factor receptor β: IC50 = 20 nM (cancer cells); Flt-3: IC50 = 57 nM (cancer cells); c-KIT: IC50 = 58 nM (cancer cells); ERK-1, MEK-1, and several other kinases: IC50 = >10 µM (cancer cells); Serine/threonine-protein kinase B-raf: EC5050 = 3 nM (human); SK-MEL-28 (Melanoma cells): EC5050 = 1300 nM (human); Vascular endothelial growth factor receptor 2: EC5050 = 500 nM (human)
Ki Data :
Vascular endothelial growth factor receptor 2: Ki= 0.021 nM (human); Serine/threonine-protein kinase B-raf: Ki= 22 nM (human)
pK Values :
pKa: 12.89, pKb: 2.66
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
216239
Merck Index :
14: 8720
MDL Number :
MFCD06411450
SMILES :
CNC(=O)C1=NC=CC(OC2=CC=C(NC(=O)NC3=CC=C(Cl)C(=C3)C(F)(F)F)C=C2)=C1

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Certificate of Analysis

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Sorafenib (CAS 284461-73-0)  Produkt Citat

See how others have used Sorafenib (CAS 284461-73-0). Click on the entry to view the PubMed entry .

Citations 1 to 10 of 80 total

PMID: # 31405179  2019. Cancers (Basel). 11:

PMID: # 30855222  Yamamoto, D.|Sato, D.|Nakayama, H.|Nakagawa, Y.|Shimada, Y.| et al. 2019. Zebrafish. 16: 233-239.

PMID: # 31149049  Chen, CY.|Wu, SM.|Lin, YH.|Chi, HC.|Lin, SL.|Yeh, CT.|Chuang, WY.|Lin, KH.| et al. 2019. Theranostics. 9: 2361-2379.

PMID: # 30659321  Di Giacomo, S.|Briz, O.|Monte, MJ.|Sanchez-Vicente, L.|Abete, L.|Lozano, E.|Mazzanti, G.|Di Sotto, A.|Marin, JJG.| et al. 2019. Arch. Toxicol. 93: 623-634.

PMID: # 30586319  Surve, SV.|Myers, PJ.|Clayton, SA.|Watkins, SC.|Lazzara, MJ.|Sorkin, A.| et al. 2019. Mol. Biol. Cell. 30: 506-523.

PMID: # 30575814  Khater, F.|Langlois, S.|Cassart, P.|Roy, AM.|Lajoie, M.|Healy, J.|Richer, C.|St-Onge, P.|Piché, N.|Perreault, S.|Cellot, S.|Marzouki, M.|Jabado, N.|Sinnett, D.| et al. 2019. Oncogene. 38: 2994-3002.

PMID: # 29551745  Khan, MA.|Ali, S.|Venkatraman, SS.|Sohail, MF.|Ovais, M.|Raza, A.| et al. 2018. Int J Pharm. 542: 196-204.

PMID: # 29040875  Marturano-Kruik, A.|Villasante, A.|Yaeger, K.|Ambati, SR.|Chramiec, A.|Raimondi, MT.|Vunjak-Novakovic, G.| et al. 2018. Biomaterials. 150: 150-161.

PMID: # 30382122  Song, Y.|Kim, IK.|Choi, I.|Kim, SH.|Seo, HR.| et al. 2018. Sci Rep. 8: 16100.

PMID: # 30140388  Schneider, T.|Martinez-Martinez, A.|Cubillos-Rojas, M.|Bartrons, R.|Ventura, F.|Rosa, JL.| et al. 2018. Oncotarget. 9: 31531-31548.

Citations 1 to 10 of 80 total
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