Sorafenib-13C,d3
Based on 1 publication(s) in Google Scholar
Sorafenib-13C,d3 (Bay 43-9006-13C,d3) is the 13C, deuterated-labeled Sorafenib (HY-10201). Sorafenib (Bay 43-9006) is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib inhibits tumor growth and metastasis in mouse and rat models. Sorafenib can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 98.35%
- CAS 番号: 1210608-86-8
- 分子式: C2013CH13D3ClF3N4O3
- 分子量:468.84
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Sorafenib-13C,d3
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Cell Proliferation/Viability Assay
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生物活性
製品説明
IC50 & Target
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VEGFR3 20 nM (IC50) |
Braf 22 nM (IC50) |
Raf-1 6 nM (IC50) |
VEGFR2 15 nM (IC50) |
BrafV599E 38 nM (IC50) |
STAT3 |
MMP2 |
Bcl-xL |
Bcl-2 |
体外実験
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
- Western Blot
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Patient-Derived Orthotopic Xenograft (PDOX)
- Protocol for Cell Cycle
- Liver Cancer Modeling
- Kinase activity and phosphorylation assays
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Autophagy
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Protocol for Kinase activity and phosphorylation assays
- Lysosome and acidic-vesicle live-cell staining
- Subcutaneous Cell-Line-Derived Xenograft
- Macroautophagy Solutions
- Orthotopic Cell-Line Xenograft
アプリケーション
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
化学情報
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CAS 番号 1210608-86-8
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非標識Cas 284461-73-0
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性状 Solid
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分子量 468.84
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分子式 C2013CH13D3ClF3N4O3
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Color Off-white to gray
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SMILES
O=C(NC(C=C1)=CC=C1OC2=CC(C(N[13C]([2H])([2H])[2H])=O)=NC=C2)NC3=CC=C(Cl)C(C(F)(F)F)=C3
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別名
Bay 43-9006-13C,d3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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BMC Cancer
IGF-1R down regulates the sensitivity of hepatocellular carcinoma to sorafenib through the PI3K / akt and RAS / raf / ERK signaling pathways. [Abstract]2023 Jan 25;23(1):87. PMID: 36698167
Sorafenib-13C,d3 purchased from MedChemExpress. Usage Cited in: BMC Cancer. 2023 Jan 25;23(1):87. [Abstract]
Sorafenib-13C,d3 (SFB; 4 µM) shows inhibition on the clone formation efficiency of HCC cells.
溶剤 & 溶解度
体外:
DMSO : 16.67 mg/mL (35.56 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
純度とドキュメンテーション
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データシート (283 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[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;64(19):7099-7109. [Content Brief]
[2]. Heim M, et al. The Raf kinase inhibitor BAY 43-9006 reduces cellular uptake of platinum compounds and cytotoxicity in human colorectal carcinoma cell lines. Anticancer Drugs. 2005;16(2):129-136. [Content Brief]
[3]. Gu FM, et al. Sorafenib inhibits growth and metastasis of hepatocellular carcinoma by blocking STAT3. World J Gastroenterol. 2011;17(34):3922-3932. [Content Brief]
[4]. El-Ashmawy NE, et al. Sorafenib effect on liver neoplastic changes in rats: more than a kinase inhibitor. Clin Exp Med. 2017;17(2):185-191. [Content Brief]
[5]. Li M, et al. Activation of an AKT/FOXM1/STMN1 pathway drives resistance to tyrosine kinase inhibitors in lung cancer. Br J Cancer. 2017;117(7):974-983. [Content Brief]
[6]. Jin W, et al. Long non-coding RNA TUC338 is functionally involved in sorafenib-sensitized hepatocarcinoma cells by targeting RASAL1. Oncol Rep. 2017;37(1):273-280. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1329 mL | 10.6646 mL | 21.3292 mL | 53.3231 mL |
| 5 mM | 0.4266 mL | 2.1329 mL | 4.2658 mL | 10.6646 mL | |
| 10 mM | 0.2133 mL | 1.0665 mL | 2.1329 mL | 5.3323 mL | |
| 15 mM | 0.1422 mL | 0.7110 mL | 1.4219 mL | 3.5549 mL | |
| 20 mM | 0.1066 mL | 0.5332 mL | 1.0665 mL | 2.6662 mL | |
| 25 mM | 0.0853 mL | 0.4266 mL | 0.8532 mL | 2.1329 mL | |
| 30 mM | 0.0711 mL | 0.3555 mL | 0.7110 mL | 1.7774 mL |
Sorafenib-13C,d3 関連分類
HY-10201S2 関連分類
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Keywords
- Sorafenib-13C,d3
- 1210608-86-8
- Bay 43-9006-13C,d3
- Isotope-Labeled Compounds
- Raf
- VEGFR
- FLT3
- Autophagy
- Apoptosis
- STAT
- Akt
- MMP
- Cadherin
- p38 MAPK
- ERK
- MEK
- PI3K
- PARP
- Bcl-2 Family
- Ephrin Receptor
- PDGFR
- c-Kit
- Raf kinases
- Vascular endothelial growth factor receptor
- Cluster of differentiation antigen 135
- CD135
- Fms like tyrosine kinase 3
- PKB
- Protein kinase B
- Matrix metalloproteinases
- Extracellular signal regulated kinases
- Mitogen-activated protein kinase kinase
- MAPKK
- MAP2K
- Phosphoinositide 3-kinase
- poly ADP ribose polymerase
- Platelet-derived growth factor receptor
- SCFR
- CD117
- VEGFR-2
- Flt-3
- c-KIT
- PI3K/Akt pathway
- MDA-MB-231 human breast carcinoma cells
- PDGFR-β
- BRAF
- RAF/MEK/ERK pathway
- Raf-1
- VEGFR-3
- Inhibitor
- inhibitor
- inhibit