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Sorafenib

In stock
Catalog No.
A3009
Raf kinases and tyrosine kinases inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$55.00
In stock
Evaluation Sample
$28.00
In stock
20mg
$105.00
In stock
50mg
$190.00
In stock
200mg
$470.00
In stock

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Sorafenib is an oral multikinase inhibitor with activity against Raf kinase and several receptor tyrosine kinases, including vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor (PDGFR), FLT3, Ret, and c-Kit. sorafenib, inhibits tumor growth and disrupts tumor microvasculature through antiproliferative, antiangiogenic, and/or proapoptotic effects. sorafenib blocks Raf kinase signaling, inhibits tumor cell proliferation, and induces apoptosis in vitro. In addition, sorafenib exhibits robust antitumor efficacy.

References

1. Sorafenib blocks the RAF/MEK/ERK pathway, inhibits tumor angiogenesis, and induces tumor cell apoptosis in hepatocellular carcinoma model PLC/PRF/5. L Liu, Y Cao, C Chen, X Zhang, A McNabola, D Wilkie  Cancer research, 2006

2. Phase II study of sorafenib in patients with advanced hepatocellular carcinoma. GK Abou-Alfa, L Schwartz, S Ricci. Journal of clinical Oncology. 2006

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt464.82
Cas No.284461-73-0
FormulaC21H16ClF3N4O3
SynonymsBAY-43-9006,Sorafenib,Nexavar,sorafenibum
Solubility≥23.25mg/mL in DMSO
Chemical Name4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]phenoxy]-N-methylpyridine-2-carboxamide
SDFDownload SDF
Canonical SMILESCNC(=O)C1=NC=CC(=C1)OC2=CC=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Protocol

Cell experiment: [1]

Cell lines

PLC/PRF/5 and HepG2 cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

IC50: 6.3 μM for PLC/PRF/5 cells 4.5 μM for HepG2 cells 72 hours

Applications

The effect of sorafenib on cell proliferation was measured by CellTiter-Glo assay. Sorafenib inhibited cell proliferation dose-dependently with an IC50 of 6.3 μmol/L in PLC/PRF/5 and 4.5 μmol/L in HepG2 cells.

Animal experiment: [1]

Animal models

Female CB17 SCID mice injected with PLC/PRF/5 cells

Dosage form

Oral administration; 10, 30, and 100 mg/kg body weight; once daily for 16 or 21 days

Applications

Sorafenib tosylate produced dose-dependent growth inhibition of s.c. implanted PLC/PRF/5 tumor xenografts in SCID mice. Dose levels of 10 and 30 mg/kg produced significant and dose-dependent TGIs of 49% and 78%, respectively. Sorafenib tosylate produced durable partial tumor regressions in 50% of the mice at the 100 mg/kg dose level.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Liu L, Cao Y, Chen C, et al. Sorafenib blocks the RAF/MEK/ERK pathway, inhibits tumor angiogenesis, and induces tumor cell apoptosis in hepatocellular carcinoma model PLC/PRF/5. Cancer research, 2006, 66(24): 11851-11858.

Biological Activity

Description Sorafenib is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively.
Targets   B-Raf VEGFR2 PDGFRβ    
IC50 6 nM 22 nM 90 nM 57 nM    

Quality Control

Chemical structure

Sorafenib

Related Biological Data

Sorafenib
Sorafenib monotherapy on inhibition of LCSC, Huh7, and PLC cells (MTT assay).

Related Biological Data

Sorafenib

Related Biological Data

Sorafenib

Related Biological Data

Sorafenib
 

Research Update

1. PKI-587 and sorafenib alone and in combination on inhibition of liver cancer stem cell proliferation. J Surg Res. 2013 Nov;185(1):225-30. doi: 10.1016/j.jss.2013.05.016. Epub 2013 May 25.
Abstract
The anti-proliferation induced by dual inhibition of PI3 K/Akt/mTOR signaling pathways and Ras/Raf/mitogen-activated protein kinase, which are associated with HCC proliferation, has been evaluated in non-liver cancer stem cell lines and LCSC lines respectively.
2. Alternative formulations of sorafenib for use in children. Pediatr Blood Cancer. 2013 Oct;60(10):1642-6. doi: 10.1002/pbc.24619. Epub 2013 Jun 20.
Abstract
Since the 200 mg tablet of sorafenib, a multikinase inhibitor with antiangiogenic and antitumor activity, is not suitable for children, extemporaneously prepared smaller-dosage of sorafenib has been investigated for stability and pharmacokinetic profile in children.
3. Sorafenib prolongs liver regeneration after hepatic resection in rats. J Surg Res. 2013 Oct;184(2):847-54. doi: 10.1016/j.jss.2013.04.062. Epub 2013 May 18.
Abstract
Sorafenib is a multikinase inhibitor that exhibits antiangiogenic and antiproliferative activity and targets signaling pathways involved in liver regeneration.
4. Iron-dependent cell death of hepatocellular carcinoma cells exposed to sorafenib. Int J Cancer. 2013 Oct 1;133(7):1732-42. doi: 10.1002/ijc.28159. Epub 2013 Apr 8.
Abstract
Sorafenib is a multikinase inhibitor that exerts cytotoxic effects on HCC cells through inducing ferroptosis, a iron-dependent and oxidative stress-associated cell death.
5. Hand-foot skin reaction is associated with the clinical outcome in patients with metastatic renal cell carcinoma treated with sorafenib. Jpn J Clin Oncol. 2013 Oct;43(10):1023-9. doi: 10.1093/jjco/hyt110. Epub 2013 Aug 15.
Abstract
The association between the Hand-Foot skin reaction and the clinical outcome in metastatic renal cell carcinoma patients treated with sorafenib were retrospectively examined.