Sorafenib

Catalog No.

A3009

Raf kinases and tyrosine kinases inhibitor

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Grouped product items
Size	Price	Stock
10mM (in 1mL DMSO)	$50.00	In stock
Evaluation Sample	$28.00	In stock
20mg	$66.00	In stock
50mg	$78.00	In stock
200mg	$163.00	In stock

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Background
Product Citation
Chemical Properties
Protocol
Biological Activity
Quality Control

Background

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 Appearance	A solid
Storage	Store at -20°C
M.Wt	464.82
Cas No.	284461-73-0
Formula	C₂₁H₁₆ClF₃N₄O₃
Synonyms	BAY-43-9006, Sorafenib, Nexavar, sorafenibum
Solubility	≥23.25 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
Chemical Name	4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]phenoxy]-N-methylpyridine-2-carboxamide
SDF	Download SDF
Canonical SMILES	CNC(=O)C1=NC=CC(=C1)OC2=CC=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F
Shipping Condition	Evaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tips	For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C 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