Sorafenib

Catalog No.S7397

Sorafenib is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM in cell-free assays, respectively.

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Sorafenib Chemical Structure

Sorafenib Chemical Structure
Molecular Weight: 464.82

Validation & Quality Control

Product Use Citation(59)

Customer Product Validation(7)

Quality Control & MSDS

Product Information

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  • Research Area
  • Inhibition Profile

Product Description

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 in cell-free assays, respectively.
Targets Raf-1 [1]
(Cell-free assay)
mVEGFR2(Flk1) [1]
(Cell-free assay)
mVEGFR3 [1]
(Cell-free assay)
B-Raf [1]
(Cell-free assay)

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IC50 6 nM 15 nM 20 nM 22 nM
In vitro Sorafenib inhibits both wild-type and V599E mutant B-Raf activity with IC50 of 22 nM and 38 nM, respectively. Sorafenib 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. Sorafenib weakly inhibits FGFR-1 with IC50 of 580 nM. Sorafenib tosylate is not active against ERK-1, MEK-1, EGFR, HER-2, IGFR-1, c-Met, PKB, PKA, cdk1/cyclinB, PKCα, PKCγ, and pim-1. Sorafenib 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. Sorafenib 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. Sorafenib inhibits the proliferation of HAoSMC and MDA-MB-231 cells with IC50 of 0.28 μM and 2.6 μM, respectively. [1] In addition to inhibition of the RAF/MEK/ERK signaling pathway, Sorafenib significantly inhibits the phosphorylation of eIF4E and down-regulates Mcl-1 levels in hepatocellular carcinoma (HCC) cells in a MEK/ERK-independent manner. Sorafenib 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. [2]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
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... Click to View More Cell Line Experimental Data

In vivo Oral administration of Sorafenib (~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, Sorafenib 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. [1] Sorafenib 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. [2] Sorafenib sensitizes bax-/- cells to TRAIL in a dose-dependent manner, through a mechanism involving down-regulating NF-κB mediated Mcl-1 and cIAP2 expression. Combining Sorafenib (30-60 mg/kg) with TRAIL (5 mg/kg) show dramatic efficacy in TRAIL-resistant HCT116 bax-/- and HT29 tumor xenografts. [3]
Features

Protocol(Only for Reference)

Kinase Assay:

[1]

Biochemical assays 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, Sorafenib tosylate is added before the enzyme initiation. A 50-fold stock plate is made with Sorafenib tosylate serially diluted 1:3 in a 50% DMSO/50% distilled water solution. Final Sorafenib tosylate concentrations range from 10 μM to 4.56 nM in 1% DMSO.

Cell Assay:

[1]

Cell lines MDA-MB-231, and HAoSMC
Concentrations Dissolved in DMSO, final concentrations ~10 μM
Incubation Time 72 hours
Method

Cells are exposed to increasing concentrations of Sorafenib tosylate for 72 hours. Cell number is quantitated using the Cell TiterGlo ATP Luminescent assay kit. This assay measures the number of viable cells per well by measurement of luminescent signal based on amount of cellular ATP.

Animal Study:

[1]

Animal Models Female NCr-nu/nu mice implanted s.c. with MDA-MB-231, Colo-205, HT-29, H460, or A549 cells
Formulation Dissolved in Cremophor EL/ethanol (50:50) as 4-fold (4 × stock solution, and diluted to 1 × with water
Dosages ~60 mg/kg
Administration Orally once daily

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Wilhelm SM, et al. Cancer Res, 2004, 64(19), 7099-7109.

[2] Liu L, et al. Cancer Res, 2006, 66(24), 11851-11858.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-05-07)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02747537 Not yet recruiting Pediatric Solid Tumors Washington University School of Medicine July 2016 Phase 2
NCT02616692 Not yet recruiting Hepatocellular Cancer Bayer May 2016 --
NCT02728050 Not yet recruiting Acute Biphenotypic Leukemia|Acute Myeloid Leukemia|de Novo Myelodysplastic Syndrome|Myeloproliferative Neoplasm University of Washington|National Cancer Institute (NCI) May 2016 Phase 1|Phase 2
NCT02691780 Not yet recruiting Refractory Solid Tumors Samsung Medical Center May 2016 --
NCT02748304 Not yet recruiting Hepatocellular Carcinoma Fudan University April 2016 --

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Chemical Information

Download Sorafenib SDF
Molecular Weight (MW) 464.82
Formula

C21H16ClF3N4O3

CAS No. 284461-73-0
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms BAY 43-9006
Solubility (25°C) * In vitro DMSO 63 mg/mL warmed (135.53 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]phenoxy]-N-methyl-pyridine-2-carboxamide

Customer Product Validation (7)


Click to enlarge
Rating
Source J Invest Dermatol 2011 131, 1886–1895. Sorafenib purchased from Selleck
Method Western blot
Cell Lines human melanoma cell lines M14 and WM-115
Concentrations 10 μM
Incubation Time 48 h
Results To see whether inhibition of this pathway has an impact on the expression of Plk-1 in human melanoma, we used specific inhibitors of mitogen-activated protein kinase kinase (MEK) 1/2 (PD98059), multikinase inhibitor (sorafenib), c-Jun N-terminal kinase (JNK) (JNK inhibitor II), and the p38 MAPK (SB203580). Treatment of human melanoma cell lines WM-115 and M14 with these inhibitors was accompanied with significant reduction of Plk-1 protein levels (Figure a). This phenomenon was accompanied by induction of apoptosis(Figure b).

Click to enlarge
Rating
Source J Neurosci 2013 33(7), 3079-93. Sorafenib purchased from Selleck
Method Immunoreactivity
Cell Lines Hair cells
Concentrations 500 nM
Incubation Time 1 h
Results To illustrate the time-dependency of JNK activation, mouse utricle and cochlea cultures were incubated for different time periods with 200 uM gentamicin, with or without a pre-incubation with 500 nM sorafenib for 1h (sorafenib was present during entire culture period). A illustrates the time-dependent activation of the JNK pathway in mouse utricles, as evident in the phosphorylation of JNK and its substrate c-Jun. In agreement with an involvement of MLK7, sorafenib nearly completely prevented JNK and c-Jun phosphorylation (B).

Click to enlarge
Rating
Source Int J Cancer 2012 10.1002/ijc.29113.. Sorafenib purchased from Selleck
Method Western blot analysis
Cell Lines A549, H460, H838 cells
Concentrations 1-3 uM
Incubation Time 48 h
Results It have therefore measured phosphorylation of AMPKa at its activation site Thr172 after treatment of cells with sorafenib, metformin or the combination thereof. A and b show an unexpected activation of AMPKa, as judged by Thr172 phosphorylation, by sorafenib treatment alone. Importantly, AMPK activation was increased significantly when sorafenib was combined with metformin, independent of LKB1 or KRAS mutation status (a and b). Increased AMPK activation was also observed when cells were treated with sorafenib in combination with the AMPK activators salicylate (c).

Click to enlarge
Rating
Source Mol Cancer Res 2014 12(10), 1377-87. Sorafenib purchased from Selleck
Method qRT-PCR
Cell Lines Tumor cells
Concentrations 1 uM
Incubation Time 24 h
Results Furthermore, siRNA-mediated knockdown of linc-VLDLR using 2 different siRNA (siRNA-linc-VLDLR-1 or siRNA-linc-VLDLR-2) decreased cell viability in response to sorafenib, doxorubicin, or camptothecin. Thus, VLDLR represents a stress-responsive lncRNA that can be induced by exposure to chemotherapy and that can contribute to acquired chemoresistance in HCC cells. We observed that linc-VLDLR was also increased in EV released from these tumor cells exposed to these anticancer agents.

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Rating
Source Mol Pharmacol 2013 84(4), 562-71. Sorafenib purchased from Selleck
Method Immunohistochemistry
Cell Lines HuH7 cells
Concentrations 25 mg/kg
Incubation Time 3 days
Results Combined exposure to sorafenib and PX-866 reduced tumor growth to a greater extent than either individual drug. Isolation of tumors at day 15 revealed that the drug combination caused morphologic alterations in the tumor (H&E staining), reduced proliferation (Ki67 staining), decreased phospho-ERK1/2 staining, and increased levels of tumor cell apoptosis (cleaved caspase 3).

Click to enlarge
Rating
Source Apoptosis 2014 19(4), 682-97. Sorafenib purchased from Selleck
Method Western blot analyses
Cell Lines HepG2 cells
Concentrations 0.1 uM
Incubation Time 1 h
Results Pretreatment with sorafenib and sunitinib reduced the LicA-induced cell death and ER stress responses, including CHOP induction, ATF6a and caspase-4 cleavage, and eIF2a phosphorylation. In contrast, sunitinib and sorafenib did not alter TG-induced cell death or ER stress responses.

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Rating
Source PLoS One 2013 8(1), e54595. Sorafenib purchased from Selleck
Method MTT assay
Cell Lines Huh7, THLE2, Hep3B cells
Concentrations 0.016-50 uM
Incubation Time 72 h
Results Cytotoxicity by sorafenib was measured by MTT assay atvarying concentrations on the HCC lines Huh7, THLE2, Hep3B.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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    GW5074 is a potent and selective c-Raf inhibitor with IC50 of 9 nM, no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms is noted.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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