Sorafenib tosylate NEW
| Price | $37 | $53 | $61 |
| Package | 50mg | 100mg | 200mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-07 |
Product Details
| Product Name: Sorafenib tosylate | CAS No.: 475207-59-1 |
| Purity: 99.81% | Supply Ability: 10g |
| Release date: 2024/11/07 |
Product Introduction
Bioactivity
| 名称 | Sorafenib tosylate |
| 描述 | Sorafenib tosylate (Bay 43-9006) is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-3/B-Raf). |
| 细胞实验 | Tumor cell lines were plated at 2 × 105 cells per well in 12-well tissue culture plates in DMEM growth media (10% heat-inactivated FCS) overnight. Cells were washed once with serum-free media and incubated in DMEM supplemented with 0.1% fatty acid-free BSA containing various concentrations of BAY 43-9006 in 0.1% DMSO for 120 minutes to measure changes in basal pMEK 1/2, pERK 1/2, or pPKB. Cells were washed with cold PBS (PBS containing 0.1 mmol/L vanadate) and lysed in a 1% (v/v) Triton X-100 solution containing protease inhibitors. Lysates were clarified by centrifugation, subjected to SDS-PAGE, transferred to nitrocellulose membranes, blocked in TBS-BSA, and probed with anti-pMEK 1/2 (Ser217/Ser221; 1:1000), anti-MEK 1/2, anti-pERK 1/2 (Thr202/Tyr204; 1:1000), anti-ERK 1/2, anti-pPKB (Ser473; 1:1000), or anti-PKB primary antibodies. Blots were developed with horseradish peroxidase (HRP)-conjugated secondary antibodies and developed with Amersham ECL reagent on Amersham Hyperfilm [1]. |
| 激酶实验 | 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 the 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. |
| 动物实验 | Female NCr-nu/nu mice (Taconic Farms, Germantown, NY) were used for all studies. Three to five million cells were injected s.c. into the right flank of each mouse. DLD-1 tumors were established and maintained as a serial in vivo passage of s.c. fragments (3 × 3 mm) implanted in the flank using a 12-gauge trocar. A new generation of the passage was initiated every three weeks, and studies were conducted between generations 3 and 12 of this line. Treatment was initiated when tumors in all mice in each experiment ranged in size from 75 to 144 mg for antitumor efficacy studies and from 100 to 250 mg for studies of microvessel density and ERK phosphorylation. All treatment was administered orally once daily for the duration indicated in each experiment. |
| 体外活性 | Besides Raf-1, Sorafenib also inhibits VEGFR-3 (IC50: 20 nM), BRAF wt (IC50: 22 nM), B-RAF V599E (IC50: 38 nM), VEGFR-2 (IC50: 90 nM), PDGFR-β (IC50: 57 nM), c-KIT (IC50: 68 nM), and Flt3 (IC50: 58 nM) in biochemical assays [1]. Sorafenib-induced phosphorylation of c-Met, p70S6K and 4EBP1 is significantly reduced when 10-0505 cells are co-treated with anti-human anti-HGF antibody, suggesting that treatment with Sorafenib leads to increased HGF secretion and activation of c-Met and mTOR targets [2]. |
| 体内活性 | Sorafenib Tosylate, administered orally at doses of 10, 30, 50, and 100 mg/kg, dose-dependently inhibits the growth of 06-0606 and 10-0505 xenograft tumors, with significant efficacy (P<0.01). Particularly, in mice, Sorafenib at 50/100 mg/kg reduces the mass of 06-0606 tumors to about 13% and 5% of untreated controls, respectively. A 50 mg dose significantly curtails tumor expansion in the 5-1318, 26-1004, and 10-0505 lines (P<0.01). With this dose, the T/C ratio—an indicator of treatment effectiveness comparing the median weights of Sorafenib-treated and control tumors—significantly declines in these xenograft models, showcasing Sorafenib's potent anti-tumor activity. Furthermore, Sorafenib improves survival rates and markedly reduces the liver index (a measure of liver enlargement) in a model of liver damage induced by Diethylnitrosamine (DENA), demonstrating enhanced survival and liver condition in treated groups compared to both DENA-exposed and normal controls. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 200 mg/mL (313.96 mM), Sonication is recommended. Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : < 1 mg/mL (insoluble or slightly soluble) 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (7.85 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. |
| 关键字 | inhibit | CD135 | Sorafenib | FLT3 | Raf kinases | Sorafenib Tosylate | Cluster of differentiation antigen 135 | Sorafenib tosylate | VEGFR | Autophagy | Ferroptosis | Raf | Inhibitor | Vascular endothelial growth factor receptor | Apoptosis | Fms like tyrosine kinase 3 |
| 相关产品 | Stavudine | Sodium 4-phenylbutyrate | L-Ascorbic acid | Hydroxychloroquine | Guanidine hydrochloride | Tributyrin | Paeonol | Naringin |
| 相关库 | 膜蛋白靶向化合物库 | 激酶抑制剂库 | EMA 上市药物库 | 酪氨酸激酶分子库 | 抗癌临床化合物库 | 药物功能重定位化合物库 | 抑制剂库 | FDA 上市激酶抑制剂库 | 抗癌上市药物库 | 抗癌活性化合物库 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
- Address: 36 Washington Street, Wellesley Hills
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