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Sorafenib

Sorafenib

产品编号 T0093L   CAS 284461-73-0
别名: 索拉非尼, Bay 43-9006

Sorafenib (Bay 43-9006) 是一种多激酶抑制剂,抑制 Raf-1、B-Raf、VEGFR2、VEGFR3、VEGFR4、PDGFRβ、FLT3、c-Kit 等 (IC50=6/22/90/15/20/20/57/58 nM),具有口服活性。Sorafenib 具有抗肿瘤活性,可以诱导细胞自噬凋亡,也可以激动铁死亡。

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Sorafenib Chemical Structure
Sorafenib, CAS 284461-73-0
规格 价格/CNY 货期 数量
5 mg ¥ 153 现货
10 mg ¥ 198 现货
25 mg ¥ 318 现货
50 mg ¥ 453 现货
100 mg ¥ 656 现货
500 mg ¥ 995 现货
1 g ¥ 1,460 现货
1 mL * 10 mM (in DMSO) ¥ 272 现货
其他形式的 Sorafenib:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
产品目录号及名称: Sorafenib (T0093L)
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纯度: 99.89%
纯度: 99.8%
纯度: 99.69%
纯度: 99.61%
纯度: 99.61%
纯度: 99%
纯度: 98.6%
纯度: 98%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Sorafenib (Bay 43-9006) is a multikinase inhibitor that inhibits Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6/22/90/15/20/20/57/58 nM) with oral activity. Sorafenib has antitumor activity and can induce autophagy and apoptosis as well as agonistic iron death.
靶点活性 c-Kit:68 nM (cell free), PDGFRβ:57 nM (cell free), B-Raf V599E:38 nM (cell free), Raf-1:6 nM (cell free0, B-Raf:22 nM (cell free), VEGFR3:20 nM (cell free)
体外活性 方法:人肝癌细胞 HepG2 和 HuH-7 用 Sorafenib (2-20 µmol/L) 处理 48 h,使用 MTT 方法检测细胞生长抑制情况。
结果:Sorafenib 剂量依赖性地抑制 HepG2 和 HuH-7 细胞生长,IC50 均约为 6 µmol/L。[1]
方法:人急性早幼粒白血病细胞 NB4 用 Sorafenib (1.5-12 µM) 处理 24-48 h,使用 Flow Cytometry 方法检测细胞凋亡情况。
结果:Sorafenib 剂量依赖性 NB4 细胞凋亡,早期和晚期凋亡细胞比例均显著增加。[2]
方法:大鼠肝胆管癌细胞 LCC-2 用 Sorafenib (2.5-5 μM) 处理 12 h,使用 JC-1 染料检测线粒体膜电位。
结果:Sorafenib 使分离的线粒体去极化。[3]
体内活性 方法:为检测体内抗肿瘤活性,将 Sorafenib (7.5-60 mg/kg) 口服给药给携带人肿瘤 MDA-MB-231、Colo-205、HT-29、DLD-1、NCI-H460 和 A549 的 NCr-nu/nu 小鼠,每天一次,持续二至四天。
结果:Sorafenib 在各种人类肿瘤异种移植物模型中显示出广泛的口服抗肿瘤功效。[4]
方法:为检测体内抗肿瘤活性,将 Sorafenib (30 mg/kg/每周五次) 和 everolimus (10 mg/kg/每周三次) 灌胃给药给携带去势抵抗性前列腺癌肿瘤 CRPC 的 PTEN 突变小鼠,每天一次,持续四周。
结果:Sorafenib 给药增加了 CRPC 中雄激素受体 p-GSK3β 和 p-ERK1/2 的表达水平。Sorafenib 和 everolimus 联合治疗克服了 CRPC 单药的治疗逃逸。[5]
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.
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].
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.
别名 索拉非尼, Bay 43-9006
化合物与蛋白结合的复合物

T0093L_1

P38 in complex with Sorafenib

分子量 464.82
分子式 C21H16ClF3N4O3
CAS No. 284461-73-0

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMF: 3.33mg/ml(7.17mM)

DMSO: 59 mg/mL (126.9 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMF / DMSO 1 mM 2.1514 mL 10.7569 mL 21.5137 mL 53.7843 mL
5 mM 0.4303 mL 2.1514 mL 4.3027 mL 10.7569 mL
DMSO 10 mM 0.2151 mL 1.0757 mL 2.1514 mL 5.3784 mL
20 mM 0.1076 mL 0.5378 mL 1.0757 mL 2.6892 mL
50 mM 0.043 mL 0.2151 mL 0.4303 mL 1.0757 mL
100 mM 0.0215 mL 0.1076 mL 0.2151 mL 0.5378 mL

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TargetMol Library Books参考文献

1. Wei JC, et al. Sorafenib inhibits proliferation and invasion of human hepatocellular carcinoma cells via up-regulation of p53 and suppressing FoxMActa Pharmacol Sin. 2015 Feb;36(2):241-51. 2. Zhang Y, et al. Sorafenib inhibited cell growth through the MEK/ERK signaling pathway in acute promyelocytic leukemia cells. Oncol Lett. 2018 Apr;15(4):5620-5626. 3. Tesori V, et al. The multikinase inhibitor Sorafenib enhances glycolysis and synergizes with glycolysis blockade for cancer cell killing. Sci Rep. 2015 Mar 17;5:9149. 4. 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. 5. Yamamoto Y, et al. Evaluation of in vivo responses of sorafenib therapy in a preclinical mouse model of PTEN-deficient of prostate cancer. J Transl Med. 2015 May 8;13:150. 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.

TargetMol Library Books文献引用

1. Wang C, Huang M, Lin Y, et al.ENO2-derived phosphoenolpyruvate functions as an endogenous inhibitor of HDAC1 and confers resistance to antiangiogenic therapy.Nature Metabolism.2023: 1-22. 2. Sun L, Wan A H, Yan S, et al.A multidimensional platform of patient-derived tumors identifies drug susceptibilities for clinical lenvatinib resistance.Acta Pharmaceutica Sinica B.2023 3. Wang X, Ji Y, Qi J, et al.Mitochondrial carrier 1 (MTCH1) governs ferroptosis by triggering the FoxO1-GPX4 axis-mediated retrograde signaling in cervical cancer cells.Cell Death & Disease.2023, 14(8): 1-13. 4. Shan X, Jiang R, Gou D, et al.Identification of a diketopiperazine‐based O‐GlcNAc transferase inhibitor sensitizing hepatocellular carcinoma to CDK9 inhibition.The FEBS Journal.2023 5. Liu M, Shi C, Song Q, et al.Sorafenib induces ferroptosis by promoting TRIM54-mediated FSP1 ubiquitination and degradation in hepatocellular carcinoma.Hepatology Communications.2023, 7(10). 6. Ni H, Ruan G, Sun C, et al. Tanshinone IIA inhibits gastric cancer cell stemness through inducing ferroptosis. Environmental Toxicology. 2021 7. Wang H, Cui Y, Gong H, et al. Suppression of AGTR1 Induces Cellular Senescence in Hepatocellular Carcinoma Through Inactivating ERK Signaling. Frontiers in Bioengineering and Biotechnology. 2022, 10. 8. Li Z, Dai H, Huang X, et al. Artesunate synergizes with sorafenib to induce ferroptosis in hepatocellular carcinoma. Acta Pharmacologica Sinica. 2020: 1-10 9. Zhang H, Xu H, Tang Q, et al. The selective serotonin reuptake inhibitors enhance the cytotoxicity of sorafenib in hepatocellular carcinoma cells. Anti-Cancer Drugs. 2021, 32(8): 793-801. 10. Feng J, Lu P, Zhu G, et al. ACSL4 is a predictive biomarker of sorafenib sensitivity in hepatocellular carcinoma. Acta Pharmacologica Sinica. 2021 Jan;42(1):160-170. doi: 10.1038/s41401-020-0439-x. Epub 2020 Jun 15.
11. Liu Y, Ouyang L, Mao C, et al. PCDHB14 promotes ferroptosis and is a novel tumor suppressor in hepatocellular carcinoma. Oncogene. 2022: 1-14 12. Xu J, Su Z, Cheng X, et al. High PPT1 expression predicts poor clinical outcome and PPT1 inhibitor DC661 enhances sorafenib sensitivity in hepatocellular carcinoma. Cancer Cell International. 2022, 22(1): 1-20. 13. Ma A, Biersack B, Goehringer N, et al. Novel Thienyl-Based Tyrosine Kinase Inhibitors for the Treatment of Hepatocellular Carcinoma. Journal of Personalized Medicine. 2022, 12(5): 738 14. Zhou J, Feng J, Wu Y, et al. Simultaneous treatment with sorafenib and glucose restriction inhibits hepatocellular carcinoma in vitro and in vivo by impairing SIAH1-mediated mitophagy. Experimental & Molecular Medicine. 2022: 1-15. 15. 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. Frontiers in Pharmacology. 2020, 10: 1646 16. Uhrig S, Ellermann J, Walther T, et al. Accurate and efficient detection of gene fusions from RNA sequencing data. Genome Research. 2021, 31(3): 448-460 17. Xu S, Liu Y, Ding Y, et al. The zinc finger transcription factor, KLF2, protects against COVID-19 associated endothelial dysfunction. Signal Transduction and Targeted Therapy. 2021, 6(1): 1-9. 18. Feng J, Lu P, Zhu G, et al. ACSL4 is a predictive biomarker of sorafenib sensitivity in hepatocellular carcinoma. Acta Pharmacologica Sinica. 2021 Jan;42(1):160-170. doi: 10.1038/s41401-020-0439-x. Epub 2020 Jun 15. 19. Fang T, Lv H, Lv G, et al. Tumor-derived exosomal miR-1247-3p induces cancer-associated fibroblast activation to foster lung metastasis of liver cancer. Nature Communications. 2018, 9(1): 1-13 20. Liu Q, Wang J, Sun H, et al.Targeting RORγ inhibits the growth and metastasis of hepatocellular carcinoma.Molecular Therapy.2024
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该产品包含在如下化合物库中:
抑制剂库 抗癌药物库 抗癌活性化合物库 膜蛋白靶向化合物库 EMA 上市药物库 抗癌临床化合物库 抗癌上市药物库 酪氨酸激酶分子库 FDA 上市激酶抑制剂库 激酶抑制剂库

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Keywords

Sorafenib 284461-73-0 Angiogenesis Apoptosis Autophagy MAPK Tyrosine Kinase/Adaptors Raf VEGFR FLT Ferroptosis PDGFR c-Kit inhibit Inhibitor CD135 Vascular endothelial growth factor receptor 索拉非尼 Fms like tyrosine kinase 3 Raf kinases Bay 43-9006 Cluster of differentiation antigen 135 FLT3 inhibitor

 

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