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ODM-203

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Chemical Structure| 1430723-35-5 同义名 : -
CAS号 : 1430723-35-5
货号 : A1173509
分子式 : C26H21F2N5O2S
纯度 : 99%+
分子量 : 505.539
MDL号 : MFCD32062783
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 65 mg/mL(128.58 mM)，配合低频超声助溶，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

  • FGFR2

    FGFR2, IC50:16 nM

  • FGFR3

    FGFR3, IC50:6 nM

  • FGFR4

    FGFR4, IC50:35 nM

  • FGFR1

    FGFR1, IC50:11 nM
描述 The FGFR family, consisting of four highly conserved receptor tyrosine kinases (FGFR 1–4), is able to directly promote endothelial cell proliferation and tumor angiogenesis. FGFR and VEGFR signaling synergistically promote tumor angiogenesis, and activation of FGFR signaling has been described as functional compensatory angiogenic signal following development of resistance to VEGFR inhibition. ODM-203 is a novel, selective, and equipotent inhibitor of the FGFR and VEGFR families with equal potency in the low nanomolar range (IC50 6 - 35 nM). ODM-203 suppressed cell proliferation in a dose-dependent manner in H1581, SNU16, and RT4 cells with IC50 values ranging from 104 nM in H1581 cells to 192 nM in RT4 cells indicating that ODM-203 can efficiently inhibit proliferation of FGFR-dependent cell lines. Moreover, ODM-203 inhibited endothelial tubule formation in a dose-dependent manner at nontoxic concentrations with an IC50 value of 33 nM. In vivo, ODM-203 showed strong antitumor activity in both FGFR-dependent xenograft models and in an angiogenic xenograft model at similar well-tolerated doses. In addition, ODM-203 inhibits metastatic tumor growth in a highly angiogenesis-dependent kidney capsule syngenic model[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.98mL

0.40mL

0.20mL

9.89mL

1.98mL

0.99mL

19.78mL

3.96mL

1.98mL
参考文献

[1]Holmström TH, Moilanen AM, Ikonen T, et al. ODM-203, a Selective Inhibitor of FGFR and VEGFR, Shows Strong Antitumor Activity, and Induces Antitumor Immunity. Mol Cancer Ther. 2019;18(1):28-38