Name: Sorafenib tosylate
Brand: Selleck Chemicals
SKU: S1040
Availability: InStock
Rating: 5 (270 reviews)

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Quality Control

Batch: Purity: 99.99%

99.99

Products Often Used Together with Sorafenib tosylate

Danusertib (PHA-739358)

It and PHA-739358 combination stops tumor growth in mice.

Related Targets	ERK p38 MAPK JNK MEK Ras KRas S6 Kinase MAP4K TAK1 Mixed Lineage Kinase
Other Raf Inhibitors	LY3009120 GDC-0879 PLX-4720 AZ 628 SB590885 TAK-632 RAF265 (CHIR-265) GW5074 Avutometinib (Ro5126766, CH5126766) PLX7904

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
MDA-MB-435	Growth Inhibition Assay	48 h	GI50=2 μM	22560627
UACC257	Growth Inhibition Assay	48 h	GI50=2 μM	22560627
MCF7	Growth Inhibition Assay	48 h	GI50=2.5 μM	22560627
EKVX	Growth Inhibition Assay	48 h	GI50=2.5 μM	22560627
HT-29	Growth Inhibition Assay	48 h	GI50=2.5 μM	22560627
SNB19	Growth Inhibition Assay	48 h	GI50=3.2 μM	22560627
OVCAR3	Growth Inhibition Assay	48 h	GI50=3.2 μM	22560627
CAKI-1	Growth Inhibition Assay	48 h	GI50=3.2 μM	22560627
SW620	Growth Inhibition Assay	48 h	GI50=3.2 μM	22560627
TK10	Growth Inhibition Assay	48 h	GI50=5 μM	22560627
endothelial precursor cells	Function assay		Inhibition of endothelial cord area formation in endothelial precursor cells by CD31 cord area detection based phenotypic drug discovery based assay, IC50 = 0.00421 μM.	22409666
Sf9	Function assay		Inhibition of GST-tagged recombinant human VEGFR2 expressed in Sf9 cells by radiometric assay, IC50 = 0.0125 μM.	24368209
endothelial precursor cells/ADSC cells	Toxicity assay		Toxicity in endothelial precursor cells co-cultured with stromal precursor ADSC cells by total nuclei count detection based phenotypic drug discovery based assay, EC50 = 5.46 μM.	22409666
endothelial precursor cells	Function assay		Inhibition of cell migration in endothelial precursor cells by Oris cell migration kit based phenotypic drug discovery based assay, IC50 = 16.7 μM.	22409666
RD	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
SK-N-SH	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
OHS-50	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 127 mg/mL (199.36 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 0.01 mg/mL

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG 300 2 5%Tween80 3 50% ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.900mg/ml (7.69mM)	Taking the 1 mL working solution as an example, add 50 μL of 98 mg/mL clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify; add 50 μL Tween-80 to the above system, mix evenly to clarify; Then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.900mg/ml (7.69mM)	Taking the 1 mL working solution as an example, add 50 μL of 98 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	637.03	Formula	C₂₁H₁₆ClF₃N₄O₃.C₇H₈O₃S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	475207-59-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	BAY 43-9006 tosylate,NSC-724772 tosylate			Smiles	CC1=CC=C(C=C1)S(=O)(=O)O.CNC(=O)C1=NC=CC(=C1)OC2=CC=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F

Mechanism of Action

Targets/IC₅₀/Ki	Raf-1 (Cell-free assay) 6 nM VEGFR2/Flk1 (Cell-free assay) 15 nM B-Raf (Cell-free assay) 22 nM B-Raf (V599E) (Cell-free assay) 38 nM PDGFRβ (Cell-free assay) 57 nM mPDGFRβ (Cell-free assay) 57 nM FLT3 (Cell-free assay) 58 nM c-Kit (Cell-free assay) 68 nM VEGFR2 (Cell-free assay) 90 nM FGFR1 (Cell-free assay) 580 nM
In vitro	Sorafenib tosylate inhibits both wild-type and V599E mutant B-Raf activity with IC50 of 22 nM and 38 nM, respectively. This compound also potently inhibits mVEGFR2 (Flk-1), mVEGFR3, mPDGFRβ, Flt3, and c-Kit with IC50 of 15 nM, 20 nM, 57 nM, 58 nM, and 68 nM, respectively. It weakly inhibits FGFR-1 with IC50 of 580 nM. This chemical is not active against ERK-1, MEK-1, EGFR, HER-2, IGFR-1, c-Met, PKB, PKA, cdk1/cyclinB, PKCα, PKCγ, and pim-1. It markedly inhibits VEGFR2 phosphorylation in NIH 3T3 cells with IC50 of 30 nM, and Flt-3 phosphorylation in HEK-293 cells with IC50 of 20 nM. It potently blocks MEK 1/2 and ERK 1/2 phosphorylation in most cell lines but not in A549 or H460 cells, while having no effect on inhibition of the PKB pathway. It inhibits the proliferation of HAoSMC and MDA-MB-231 cells with IC50 of 0.28 μM and 2.6 μM, respectively. In addition to inhibition of the RAF/MEK/ERK signaling pathway, it significantly inhibits the phosphorylation of eIF4E and down-regulates Mcl-1 levels in hepatocellular carcinoma (HCC) cells in a MEK/ERK-independent manner. It inhibits the proliferation of PLC/PRF/5 and HepG2 cells with IC50 of 6.3 μM and 4.5 μM, respectively, and leads to the significant induction of apoptosis.
Kinase Assay	Biochemical assays
Kinase Assay	Recombinant baculoviruses expressing Raf-1 (residues 305–648) and B-Raf (residues 409–765) are purified as fusion proteins. Full-length human MEK-1 is generated by PCR and purified as a fusion protein from Escherichia coli lysates. Sorafenib tosylate is added to a mixture of Raf-1 (80 ng), or B-Raf (80 ng) with MEK-1 (1 μg) in assay buffer [20 mM Tris (pH 8.2), 100 mM NaCl, 5 mM MgCl₂, and 0.15% β-mercaptoethanol] at a final concentration of 1% DMSO. The Raf kinase assay (final volume of 50 μL) is initiated by adding 25 μL of 10 μM γ[³³P]ATP (400 Ci/mol) and incubated at 32 °C for 25 minutes. Phosphorylated MEK-1 is harvested by filtration onto a phosphocellulose mat, and 1% phosphoric acid is used to wash away unbound radioactivity. After drying by microwave heating, a β-plate counter is used to quantify filter-bound radioactivity. Human VEGFR2 (KDR) kinase domain is expressed and purified from Sf9 lysates. Time-resolved fluorescence energy transfer assays for VEGFR2 are performed in 96-well opaque plates in the time-resolved fluorescence energy transfer format. Final reaction conditions are as follows: 1 to 10 μM ATP, 25 nM poly GT-biotin, 2 nM Europium-labeled phospho (p)-Tyr antibody (PY20), 10 nM APC, 1 to 7 nM cytoplasmic kinase domain in final concentrations of 1% DMSO, 50 mM HEPES (pH 7.5), 10 mM MgCl₂, 0.1 mM EDTA, 0.015% Brij-35, 0.1 mg/mL BSA, and 0.1% β-mercaptoethanol. Reaction volumes are 100 μL and are initiated by addition of enzyme. Plates are read at both 615 and 665 nM on a Perkin-Elmer VictorV Multilabel counter at ~1.5 to 2.0 hours after reaction initiation. Signal is calculated as a ratio: (665 nm/615 nM) × 10,000 for each well. For IC50 generation, this compound is added before the enzyme initiation. A 50-fold stock plate is made with this chemical serially diluted 1:3 in a 50% DMSO/50% distilled water solution. Final concentrations of this compound range from 10 μM to 4.56 nM in 1% DMSO.
In vivo	Oral administration of Sorafenib tosylate (~60 mg/kg) demonstrates broad spectrum, dose-dependent anti-tumor activity against a variety of human tumor xenograft models including MDA-MB-231, Colo-205, HT-29, DLD-1, NCI-H460, and A549, with no evidence of toxicity. In association with the anti-tumor efficacy, this compound treatment potently inhibits MEK 1/2 phosphorylation and pERK 1/2 levels in HT-29 and MDA-MB-231 xenografts but not in Colo-205 xenografts, and significantly suppresses tumor microvessel area (MVA) and microvessel density (MVD) in MDA MB-231, HT-29 and Colo-205 tumor xenografts. This compound treatment produces dose-dependent growth inhibition of PLC/PRF/5 tumor xenografts in SCID mice with TGIs of 49% and 78% at 10 mg/kg and 30 mg/kg, respectively, consistent with the inhibition of ERK and eIF4E phosphorylation, reduction of the microvessel area, and induction of tumor cell apoptosis.
References	[1] https://pubmed.ncbi.nlm.nih.gov/15466206/ [2] https://pubmed.ncbi.nlm.nih.gov/17178882/ [3] https://pubmed.ncbi.nlm.nih.gov/17613437/

Applications

Methods	Biomarkers	PMID
Western blot	LC3-I / LC-3II / ATG5 p-STAT3 / STAT3/ Mcl-1 β-catenin / Survivin / Mcl-1 / PTMA pERK / ERK p-PKM2(Y105) / PMK2 / Caspase-9 RET(pY1016) / VEGFR2(pY1214) / MEK1(pT292) / ERK(pY204) Cyclin D1	23392173
Immunofluorescence	p65 cytochrome c	22286758
Growth inhibition assay	Cell viability	26039995
ELISA	TGF-beta / CD206 Caspase-9 / Caspase-3	26158762

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05068752	Recruiting	Pancreas Cancer	HonorHealth Research Institute\|Bayer\|Genentech Inc.	October 28 2021	Phase 2
NCT04763408	Active not recruiting	Carcinoma Hepatocellular	Eisai Inc.	April 9 2021	--

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Sorafenib tosylate Raf inhibitor

Chemical Structure

Molecular Weight: 637.03