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MAPK Raf Sorafenib

Sorafenib

Catalog No. T0093L   CAS 284461-73-0
Synonyms: Bay 43-9006

Sorafenib is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-4/B-Raf).

Sorafenib, CAS 284461-73-0
Pack Size Availability Price/USD Quantity
2 mg In stock 12.00
10 mg In stock 20.00
50 mg In stock 41.00
100 mg In stock 50.00
500 mg In stock 75.00
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Purity 99.89%
Purity 99.00%
Purity 99.69%
Purity 98.60%
Purity 98.00%
Purity 99.15%
Biological Description
Chemical Properties
Storage & Solubility Information
Description Sorafenib is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-4/B-Raf).
Targets&IC50 B-Raf : ic50 22nM ,   B-Raf (V599E) : ic50 38nM ,   Raf-1 : ic50 6nM ,   VEGFR2/Flk1 : ic50 15nM ,   VEGFR3 : ic50 20nM
In vivo Sorafenib Tosylate (10, 30, 50 and 100 mg/kg, p.o.) inhibits the tumor growth of 06-0606 and 10-0505 xenografts in a dose-dependent manner (P<0.01). The growth rate of 06-0606 and 10-0505 xenografts is also significantly reduced by Sorafenib. The weights of 06-0606 tumors in mice that are treated with Sorafenib (50/100 mg/kg) are approximately 13% and 5% of the controls, respectively. 50 mg dose of Sorafenib significantly inhibits tumor growth in mice with lines 5-1318, 26-1004 and 10-0505 (P<0.01). For 50 mg dose, the T/C ratio, where T and C are the median weight (mg) of Sorafenib- and vehicle-treated tumors at the end of the treatment, respectively, for 06-0606, 26-1004, 5-1318, and 10-0505 xenografts is 0.13, 0.10, 0.12 and 0.49, respectively [2]. The survival rate is 73.3 % in Diethylnitrosamine (DENA) group and 83.3 % in the Sorafenib group compared to 100 % in the normal control group. DENA group shows a significant increase in the liver index (1.51-fold increase, p<0.05) compared to normal control group, while treatment with Sorafenib shows a significant decrease (p<0.05) in the liver index when compared to DENA group. The liver index in Sorafenib group significantly decreases to lower than its value in the normal control [3].
Kinase Assay 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 Research
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. (Only for Reference)
Cell lines: MDA-MB-231, and HAoSMC
Animal Research
Animal Model: FeNCr-nu/nu mice implanted s.c. with MDA-MB-231, Colo-205, HT-29, H460, or A549 cells
Synonyms Bay 43-9006
Purity 99.89%
Molecular Weight 464.83
Formula C21H16ClF3N4O3
CAS No. 284461-73-0

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 59 mg/mL (126.9 mM)

Ethanol: <1 mg/mL

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Wilhelm SM, et al. BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis. Cancer Res. 2004 Oct 1;64(19):7099-109. 2. Huynh H, et al. Sorafenib and rapamycin induce growth suppression in mouse models of hepatocellular carcinoma. J Cell Mol Med. 2009 Aug;13(8B):2673-83. 3. El-Ashmawy NE, et al. Sorafenib effect on liver neoplastic changes in rats: more than a kinase inhibitor. Clin Exp Med. 2016 Apr 16. 4. Bai C, Sun Y, Pan X, et al. Antitumor Effects of Trimethylellagic Acid Isolated From Sanguisorba officinalis L. on Colorectal Cancer via Angiogenesis Inhibition and Apoptosis Induction[J]. Frontiers in Pharmacology. 2020, 10: 1646. 5. Feng J, Lu P, Zhu G, et al. ACSL4 is a predictive biomarker of sorafenib sensitivity in hepatocellular carcinoma[J]. Acta Pharmacologica Sinica. 2020: 1-11. 6. Li Z, Dai H, Huang X, et al. Artesunate synergizes with sorafenib to induce ferroptosis in hepatocellular carcinoma[J]. Acta Pharmacologica Sinica. 2020: 1-10. 7. Uhrig S, Ellermann J, Walther T, et al. Accurate and efficient detection of gene fusions from RNA sequencing data[J]. Genome Research. 2021 8. Fang, Tian, et al. Tumor-derived exosomal miR-1247-3p induces cancer-associated fibroblast activation to foster lung metastasis of liver cancer. Nature communications. 2018 Jan 15;9(1):191.

Related compound libraries

This product is contained In the following compound libraries:
Approved Drug Library Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Autophagy Compound Library Neuronal Signaling Compound Library MAPK Inhibitor Library Tyrosine kinase inhibitor library FDA-approved Drug Library Cytokine Inhibitor Library Kinase Inhibitor Library Anti-cancer Approved drug Library Fluorochemical Library Angiogenesis related Compound Library CNS-Penetrant Compound Library

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