Sorafenib Sorafenib is a RAF kinase which suppresses ERK phosphorylation. It also inhibits other kinases such as Flk-1 (VEGFR2), PDGFR, FLT3, Ret, and c-Kit.

Sorafenib (CAS 284461-73-0)

Sorafenib | CAS 284461-73-0 is rated 5.0 out of 5 by 2.
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| See product citations (11)
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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Ordering Information

PRODUCT NAME CATALOG # UNIT PRICE QTY FAVORITES
Sorafenib sc-220125 5 mg $50.00
Sorafenib sc-220125A 50 mg $250.00

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

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
Boiling Point :
~523.35° C at 760 mmHg (Predicted)
Density :
~1.5 g/cm3 (Predicted)
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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SorafenibProduct Citations

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

Citations 1 to 10 of 11 total

PMID: # 28327152
Mastropasqua, F. et al. 2017. TRIM8 restores p53 tumour suppressor function by blunting N-MYC activity in chemo-resistant tumours. Mol. Cancer. 16: 67.

PMID: # 28404959
Zheng, M. et al. 2017. Inhibition of the prolyl isomerase Pin1 enhances the ability of sorafenib to induce cell death and inhibit tumor growth in hepatocellular carcinoma. Oncotarget. 8: 29771-29784.

PMID: # 26929621
Petrushev, B. et al. 2016. Gold nanoparticles enhance the effect of tyrosine kinase inhibitors in acute myeloid leukemia therapy. Int J Nanomedicine. 11: 641-60.

PMID: # 26100943
Mani, J. et al. 2016. Knockdown of BAG3 sensitizes bladder cancer cells to treatment with the BH3 mimetic ABT-737. World J Urol. 34: 197-205.

PMID: # 26808072
Suarasan, S. et al. 2016. Gelatin-coated Gold Nanoparticles as Carriers of FLT3 Inhibitors for Acute Myeloid Leukemia Treatment. Chem Biol Drug Des. 87: 927-35.

PMID: # 26625890
Simon, T. et al. 2015. Design of FLT3 Inhibitor - Gold Nanoparticle Conjugates as Potential Therapeutic Agents for the Treatment of Acute Myeloid Leukemia. Nanoscale Res Lett. 10: 466.

Sprinzl, MF. et al. 2015. Sorafenib inhibits macrophage-induced growth of hepatoma cells by interference with insulin-like growth factor-1 secretion. J. Hepatol.. 62: 863-70.

PMID: # 26158762
Wei, X. et al. 2015. MiR-101 targets DUSP1 to regulate the TGF-β secretion in sorafenib inhibits macrophage-induced growth of hepatocarcinoma. Oncotarget. 6: 18389-405.

PMID: # 26301220
Pallegar, NK. et al. 2015. Repression of CD24 surface protein expression by oncogenic Ras is relieved by inhibition of Raf but not MEK or PI3K. Front Cell Dev Biol. 3: 47.

PMID: # 23785399
Kwon, JH. et al. 2013. Actionable gene expression-based patient stratification for molecular targeted therapy in hepatocellular carcinoma. PLoS ONE. 8: e64260.

Citations 1 to 10 of 11 total

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: 2017-05-19

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: 2017-04-11

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: 2017-04-11

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: 2016-12-15

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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