Sulfatinib

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Chemical Structure| 1308672-74-3 同义名 : 索凡替尼 ;Surufatinib;HMPL-012;Surfatinib;Sufatinib
CAS号 : 1308672-74-3
货号 : A287603
分子式 : C24H28N6O3S
纯度 : 99+%
分子量 : 480.582
MDL号 : -
存储条件：

Pure form Keep in dark place,Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(218.48 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • FGFR1

    FGFR1, IC50:15 nM
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.08mL

0.42mL

0.21mL

10.40mL

2.08mL

1.04mL

20.81mL

4.16mL

2.08mL
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.