生物活性

• 靶点

  VEGFR2 IC50:0.021μM

  FGFR1 IC50:0.053μM

• 描述The inhibition of VEGFR-, FGFR-, and CSF1R-mediated pathways may be an effective approach to prevent tumor angiogenesis and immune evasion. Sulfatinib is a potent, small molecule tyrosine kinase inhibitor of VEGFR1, VEGFR2, VEGFR3, FGFR1, and CSF1R with IC50 values of 2, 24, 1, 15, and 4 nM, respectively. It also demonstrated selectivity against fms-related tyrosine kinase 3 and tropomyosin receptor kinase B with IC50 values of 41 and 67 nM, respectively^[2]. Sulfatinib inhibited VEGF-induced VEGFR2 phosphorylation in HEK293KDR cells and CSF-1R phosphorylation in RAW264.7 cells with IC50 values of 2 and 79 nM, respectively. It also suppressed VEGF- or FGF-induced proliferation of human umbilical vein endothelial cells with an IC50 less than 50 nM. In nude mice, a single oral dose of sulfatinib inhibited VEGF-stimulated VEGFR2 phosphorylation in lung tissues and suppressed FGFR signaling as evidenced by the upregulation of FGF23 in the plasma^[3].
• 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
  NCT02588170	Neuroendocrine Tumors	Phase 3	Recruiting	December 2019	China, Beijing ... more >> Peking Union Medical College Hospital Not yet recruiting Beijing, Beijing, China, 100032 Contact: Chunmei Bai, Prof.       baichunmei1964@163.com    Principal Investigator: Chunmei Bai, Prof.          the 307 Hospital of People's Liberation Army Recruiting Beijing, Beijing, China, 100071 Contact: Jianming XU, Prof.       jmxu2003@yahoo.com    Principal Investigator: Jianming XU, Prof.          Beijing Cancer Hospital Recruiting Beijing, Beijing, China, 100142 Contact: Jie Li, Prof.       xiaotong10241@sina.com    Principal Investigator: Jie Li, Prof.          China, Guangdong Sun Yat-sen University Cancer Center Recruiting Guangzhou, Guangdong, China, 510060 Contact: Zhiwei Zhou, Prof.       zhouzhw@sysucc.org.cn    Principal Investigator: Zhiwei Zhou, Prof.          China, Sichuan West China Hospital, Sichuan University Recruiting Chengdu, Sichuan, China, 610047 Contact: Zhiping Li, Prof.       lizhiping620312@163.com    Principal Investigator: Zhiping Li, Prof. Collapse <<
  NCT02614495	Thyroid Carcinoma	Phase 2	Recruiting	July 2019	China, Beijing ... more >> Peking Union Medical College Hospital Not yet recruiting Beijing, Beijing, China, 100032 Contact: Chunmei Bai, Prof.       baichunmei1964@163.com    Principal Investigator: Chunmei Bai, Prof.          China, Shanghai Fudan University Shanghai Cancer Center Recruiting Shanghai, Shanghai, China, 200032 Contact: Qinghai Ji, Prof.       jiqinghai@shca.org.cn    Principal Investigator: Qinghai Ji, Prof. Collapse <<
  NCT02966821	Biliary Tract Cancer	Phase 2	Active, not recruiting	May 2019	China, Beijing ... more >> Peking Union Medical College Hospital Beijing, Beijing, China, 100032 The 307th Hospital of Military Chinese People's Liberation Army Beijing, Beijing, China, 100071 China, Heilongjiang Heilongjiang Cancer Hospital Ha'erbin, Heilongjiang, China, 150040 China, Shanghai Shanghai Zhongshan Hospital Shanghai, Shanghai, China, 200032 China, Tianjin Tianjin medical university cancer institute&hospital Tianjin, Tianjin, China, 300060 Collapse <<

• 更多
• 参考文献

• [1] Xu JM, Wang Y, et al. Sulfatinib, a novel kinase inhibitor, in patients with advanced solid tumors: results from a phase I study. Oncotarget. 2017 Jun 27;8(26):42076-42086.

  [2] Xu JM, Wang Y, Chen YL, et al. Sulfatinib, a novel kinase inhibitor, in patients with advanced solid tumors: results from a phase I study. Oncotarget. 2017;8(26):42076-42086. doi:10.18632/oncotarget.14942

  [3] Sulfatinib Pre-clinical Evidence.