SorafenibAn inhibitor of tyrosine protein kinases that targets the Raf/Mek/Erk pathway

Sorafenib (CAS 284461-73-0)

Sorafenib | CAS 284461-73-0 is rated 5.0 out of 5 by 2.
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Synonym: Nexavar; Sorafenibum; BAY 43-9006
Application: An inhibitor of tyrosine protein kinases that targets the Raf/Mek/Erk pathway
CAS Number: 284461-73-0
Purity: ≥99%
Molecular Weight: 464.82
Molecular Formula: C21H16ClF3N4O3
* Refer to Certificate of Analysis for lot specific data (including water content).
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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.


References

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), Hot Methanol, DMF (~20 mg/ml), 1:2 solution of DMSO:PBS(PH 7.2 ) (~0.3 mg/ml), 100% ethanol, and ethyl acetate.
Storage :
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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Sorafenib  Product Citations

See how others have used Sorafenib. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 64 total

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

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

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

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: # 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: # 29864454  Liang, YY.|Deng, XB.|Zeng, LS.|Lin, XT.|Shao, XF.|Wang, B.|Mo, ZW.|Yuan, YW.| et al. 2018. Cancer Lett. 432: 75-83.

PMID: # 29801504  Song, Y.|Kim, JS.|Kim, SH.|Park, YK.|Yu, E.|Kim, KH.|Seo, EJ.|Oh, HB.|Lee, HC.|Kim, KM.|Seo, HR.| et al. 2018. J. Exp. Clin. Cancer Res. 37: 109.

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

PMID: # 29805309  Xie, L.|Zeng, Y.|Dai, Z.|He, W.|Ke, H.|Lin, Q.|Chen, Y.|Bu, J.|Lin, D.|Zheng, M.| et al. 2018. Int. J. Biol. Sci. 14: 577-585.

Citations 1 to 10 of 64 total

For in vivo use, a lot of literature has stated sorafenib needs to be dissolved in a cremaphor solution (one example is 30% (w/v) cremophor, 30% (w/v) PEG 400, 10% ethanol, and 10% glucose). Do you have any information about this solution for solubility.

Asked by: avila
Thank you for your question. Sorafenib (CAS 284461-73-0) sc-220125 is soluble in DMSO (~20 mg/ml), Hot Methanol, DMF (~20 mg/ml), 1:2 solution of DMSO:PBS(PH 7.2 ) (~0.3 mg/ml), 100% ethanol, and ethyl acetate. If you require additional information on this compound please get in touch with technical service.
Answered by: Tech Support Europe
Date published: 2019-07-04

Does a solution of Sorafenib in DMSO interact with DMEM or Fetal Bovine Serum? and If not, what is the storage conditions for such solution (Sorafenib plus DMEM plus FBS)? Thanks a lot

Asked by: Ahmed Abdelmageed Saad
Thank you for your question. We have not tested this, so we cannot comment on the interaction with DMEM or FBS. We always recommend using solutions the same day they are made. However, if necessary to make ahead of time, solutions should be stored at -20ºC.
Answered by: Technical Service
Date published: 2018-11-14

What is the stability of Sorafenib (sc-220125) at room temperature? and what is the perfect transportation condition?

Asked by: Ahmed Abdelmageed Saad
Thank you for your question. We transport Sorafenib (sc-220125) at room temperature and we don’t recommend storing at room temperature for longer than 2 weeks.
Answered by: Technical Support
Date published: 2018-11-14

Could you please tell me what the storage conditions are after solubilisation in DMSO and how long can I store them? 

Asked by: two2igm05
Thank you for your question. Sorafenib, sc-220125, can be stored for 6 months at -80℃ in solvent.
Answered by: TechService7
Date published: 2019-08-12

What is the solubility of this product?

Asked by: hawkeye11
Thank you for you question. This product is soluble in DMSO (~20 mg/ml), warm methanol (<1 mM), 1:2 solution of PBS:DMSO (.3 mg/ml), and in ethanol. Please contact Technical Service if you have further questions concerning this product.
Answered by: Tech Service 9
Date published: 2018-08-07

I would like to ask a quotation on the following drug. CAS number: 284461-73-0 Cat number: sc-220125A Name: Sorafenib (pure) Quantity: 100mg I would appreciate if you could include the shipping costs in the quotation Regards Alexandra Alvarez

Asked by: lexalfer
Thank you for your inquiry with Santa Cruz Biotechnology. For an accurate quote with pricing and shipping information, please contact one of our authorized distributors in Singapore. You can find their contact information here: https://www.scbt.com/scbt/resources/distributors
Answered by: Tech Service
Date published: 2016-10-05
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Rated 5 out of 5 by from Shows strong inhibition of Ras/ERK pathway at 1uM Shows strong inhibition of Ras/ERK pathway at 1uM, leading to decreased migration in C6 cells.
Date published: 2015-04-08
Rated 5 out of 5 by from A lack of phosphorylation of the ERK protein A lack of phosphorylation of the ERK protein was observed by WB using SK-MEL-28 cells post treatment with Sorafenib. -SCBT QC
Date published: 2015-03-23
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