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首页 / 抑制剂/激动剂 / 蛋白质酪氨酸激酶(Protein Tyrosine Kinase) / c-Met/HGFR / Tivantinib

Tivantinib {[allProObj[0].p_purity_real_show]}

货号：A891951 同义名： ARQ 197; (3R,4R)-ARQ 198

Tivantinib is an non-ATP-competitive c-Met inhibitor with Ki of 0.355 μM with little activity to Ron, and no inhibition to EGFR, InsR, PDGFRα or FGFR1/4.

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Tivantinib 化学结构 CAS号：905854-02-6
Tivantinib 化学结构
CAS号：905854-02-6
Tivantinib 3D分子结构
CAS号：905854-02-6
Tivantinib 化学结构 CAS号：905854-02-6
Tivantinib 3D分子结构 CAS号：905854-02-6
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Tivantinib 纯度/质量文件 产品仅供科研

货号：A891951 标准纯度： {[allProObj[0].p_purity_real_show]}
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Tivantinib 生物活性

描述 The receptor tyrosine kinase, MET proto-oncogene, receptor tyrosine kinase (c-MET) is a high-affinity receptor for hepatocyte growth factor (HGF), and its downstream v-akt murine thymoma viral oncogene homolog (AKT) and mitogen-activated protein kinase (ERK) pathways are regulated by HGF/c-MET. The HGF/c-MET axis is involved in cancer progression, metastasis, and acquired resistance[3]. HGF/c-MET signaling is often highly activated in tumors because of various mechanisms. MET is a high-affinity tyrosine kinase receptor (RTK) for hepatocyte growth factor (HGF). HGF binding triggers the dimerization of MET receptors, then activation of multiple intracellular pathways such as mitogen-activated protein kinase (MAPK), phosphatidylinositol 3-kinase (PI3K) and focal adhesion kinase (FAK). Tivantinib (ARQ-197) inhibits MET by binding to the inactive conformation of MET to stabilize this conformation. This prevents MET phosphorylation and dampens downstream signaling, thereby resulting in growth inhibition and induction of apoptosis in solid tumors. Tivantinib can induce a G2/M arrest and promoted apoptosis by both intrinsic and extrinsic pathway. Tivantinib is a highly selective, orally administered, non-ATP competitive inhibitor of the MET, with an inhibitory constant (Ki) of 355 nM[4]. Tivantinib also inhibited constitutive p-MET and HGF-induced p-MET in several type of tumor cells with an IC50 of 100 to 300 nM. In vivo experiment, MHCC97L xenograft mice were treated daily with an oral dose of tivantinib at 100 mg/kg or 200 mg/kg for 15 days. Tivantinib displayed a good anti-tumor effect on MHCC97L xenografts and tumor growth inhibition (TGI) rates were 30.9% and 64.6%, respectively[4]. In vivo study, EBC-1 cells were treated with the indicated concentrations of Tivantinib and incubated concentrations ranging from 1-10μM for another 72h. It was found that tivantinib treatment inhibited tubulin polymerization in a concentration-dependent manner but did not inhibit c-MET and its downstream AKT and ERK signaling pathways[3].
作用机制 Tivantinib(ARQ-197) inhibits MET by binding to the inactive conformation of MET to stabilize this conformation.

Tivantinib 细胞研究

细胞系 浓度 检测类型 检测时间 活性说明 数据源
1833/TGL ~100 μM Growth inhibitory assay GI50=3.7 μM 22027690
697 10 μM Growth inhibitory assay EC50=338 nM 19064730
786-0 10 μM Growth inhibitory assay IC50=4009 nM 18381444
786-0 10 μM Kinase assay inhibits pGSK3β with IC50 of 150 nM 18381444

Tivantinib 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00557609 Renal Cell Carcinoma (RCC) ... 展开 >> Alveolar Soft Part Sarcoma (ASPS) Clear Cell Sarcoma (CCS) 收起 << Phase 2 Completed - United States, California ... 展开 >> San Francisco, California, United States, 94143 Santa Monica, California, United States, 90404 United States, Florida Miami, Florida, United States, 33136 United States, Massachusetts Boston, Massachusetts, United States, 02115 United States, Ohio Cincinnati, Ohio, United States, 45229 United States, Texas Dallas, Texas, United States, 75201 Houston, Texas, United States, 77030 Canada, Ontario Toronto, Ontario, Canada, M5G 2M9 United Kingdom London, United Kingdom, SW3 6JJ 收起 <<
NCT01696955 Head and Neck Squamous Cell Ca... 展开 >>rcinoma Recurrent Head and Neck Carcinoma 收起 << Phase 2 Active, not recruiting - United States, Arizona ... 展开 >> Mayo Clinic in Arizona Scottsdale, Arizona, United States, 85259 United States, California City of Hope Comprehensive Cancer Center Duarte, California, United States, 91010 USC / Norris Comprehensive Cancer Center Los Angeles, California, United States, 90033 University of California Davis Comprehensive Cancer Center Sacramento, California, United States, 95817 City of Hope South Pasadena South Pasadena, California, United States, 91030 United States, Illinois Northwestern University Chicago, Illinois, United States, 60611 University of Chicago Comprehensive Cancer Center Chicago, Illinois, United States, 60637 Decatur Memorial Hospital Decatur, Illinois, United States, 62526 NorthShore University HealthSystem-Evanston Hospital Evanston, Illinois, United States, 60201 Ingalls Memorial Hospital Harvey, Illinois, United States, 60426 Illinois CancerCare-Peoria Peoria, Illinois, United States, 61615 Southern Illinois University School of Medicine Springfield, Illinois, United States, 62702 United States, Indiana Fort Wayne Medical Oncology and Hematology Inc-Parkview Fort Wayne, Indiana, United States, 46845 Indiana University/Melvin and Bren Simon Cancer Center Indianapolis, Indiana, United States, 46202 United States, Iowa University of Iowa/Holden Comprehensive Cancer Center Iowa City, Iowa, United States, 52242 United States, Maryland University of Maryland/Greenebaum Cancer Center Baltimore, Maryland, United States, 21201 United States, Michigan University of Michigan Comprehensive Cancer Center Ann Arbor, Michigan, United States, 48109 Wayne State University/Karmanos Cancer Institute Detroit, Michigan, United States, 48201 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 Metro Minnesota Community Oncology Research Consortium Saint Louis Park, Minnesota, United States, 55416 United States, Missouri Washington University School of Medicine Saint Louis, Missouri, United States, 63110 Mercy Hospital Saint Louis Saint Louis, Missouri, United States, 63141 United States, Pennsylvania Penn State Milton S Hershey Medical Center Hershey, Pennsylvania, United States, 17033-0850 University of Pittsburgh Cancer Institute (UPCI) Pittsburgh, Pennsylvania, United States, 15232 收起 <<
NCT01468922 Sarcoma Stoma... 展开 >>ch Neoplasms Neoplasms 收起 << Phase 1 Completed - United States, Maryland ... 展开 >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 收起 <<

Tivantinib 参考文献

[1]Munshi N, Jeay S, et al. ARQ 197, a novel and selective inhibitor of the human c-Met receptor tyrosine kinase with antitumor activity. Mol Cancer Ther. 2010 Jun;9(6):1544-53.

[2]Comoglio PM, Giordano S, et al. Drug development of MET inhibitors: targeting oncogene addiction and expedience. Nat Rev Drug Discov. 2008 Jun;7(6):504-16.

[3]Aoyama A, Katayama R, Oh-Hara T, Sato S, Okuno Y, Fujita N. Tivantinib (ARQ 197) exhibits antitumor activity by directly interacting with tubulin and overcomes ABC transporter-mediated drug resistance. Mol Cancer Ther. 2014 Dec;13(12):2978-90. doi: 10.1158/1535-7163.MCT-14-0462. Epub 2014 Oct 13. PMID: 25313010.

[4]Xiang Q, Zhen Z, Deng DY, Wang J, Chen Y, Li J, Zhang Y, Wang F, Chen N, Chen H, Chen Y. Tivantinib induces G2/M arrest and apoptosis by disrupting tubulin polymerization in hepatocellular carcinoma. J Exp Clin Cancer Res. 2015 Oct 12;34:118. doi: 10.1186/s13046-015-0238-2. PMID: 26458953; PMCID: PMC4603939.

Tivantinib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.71mL

0.54mL

0.27mL

13.53mL

2.71mL

1.35mL

27.07mL

5.41mL

2.71mL

Tivantinib 技术信息

CAS号905854-02-6
分子式C23H19N3O2
分子量 369.42
SMILES Code O=C([C@@H](C1=CN2CCCC3=C2C1=CC=C3)[C@@H]4C5=CNC6=C5C=CC=C6)NC4=O
MDL No. MFCD11977597
别名 ARQ 197; (3R,4R)-ARQ 198
运输蓝冰
InChI Key UCEQXRCJXIVODC-PMACEKPBSA-N
Pubchem ID 11494412
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere, store in freezer, under -20°C

Tags: Tivantinib | ARQ 197;(3R,4R)-ARQ 198;​ARQ 197 | c-Met/HGFR | AmBeed-信号通路专用抑制剂 | Tivantinib 纯度/质量文件 | Tivantinib 生物活性 | Tivantinib 细胞研究 | Tivantinib 临床数据 | Tivantinib 参考文献 | Tivantinib 实验方案 | Tivantinib 技术信息

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