ODM-203
目录号: PL02396 纯度: ≥99%
CAS No. :1430723-35-5
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中文名称
ODM-203
中文别名
N-(2' ,4'-二氟-5-(5-(1-甲基-1H-吡唑-4-基)-1H-苯并[d]咪唑-1-基)-[1,1'-联苯]-3-基)环丙烷磺酰胺
英文名称
ODM-203
英文别名
ZJFCBQXPTQSTCZ-UHFFFAOYSA-N;BDBM247327;s8882;US9447091, 5;N-(2',4'-difluoro-5-(5-(1-methyl-1H-pyrazol-4-yl)-1H-benzo[d]imidazol-1-yl)-biphenyl-3-yl)cyclopropanesulfonamide;N-[3-(2,4-Difluorophenyl)-5-[5-(1-methylpyrazol-4-yl)benzimidazol-1-yl]phenyl]cyclopropanesulfonamid;ODM-203
Cas No.
1430723-35-5
分子式
C26H21F2N5O2S
分子量
505.54
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
ODM-203 是一种口服有效的,具有选择性的 FGFR/VEGFR 抑制剂,其对 FGFR3/1/2 和 VEGFR3/2/1/4 的 IC50 值分别为 6, 11, 16, 5, 9, 26 和 35 nM。ODM-203 具有很强的抗肿瘤活性,并能激活肿瘤微环境中的免疫反应。
生物活性
ODM-203 is an orally active and selective FGFR/VEGFR inhibitor with IC 50 values of 6, 11, 16, 5, 9, 26 and 35 nM for FGFR3/1/2 and VEGFR3/2/1/4, respectively. ODM-203 has strong anti-tumour activity and activates immune responses in the tumour microenvironment.
性状
Solid
IC50 & Target[1][2]
FGFR1 11 nM (IC50) FGFR2 16 nM (IC50
体外研究(In Vitro)
ODM-203 (eight-dose concentration series up to 3 μM; 96 h) potently inhibits FGFR signaling and proliferation in several FGFR-dependent cell lines.
ODM-203 (eight-dose concentration series up to 3 μM; 10 days) inhibits endothelial tubule formation.
ODM-203 (1, 10, 100, 1000 nM; 1 h) inhibiting FGFR and VEGFR cellular signaling in HUVEC cells. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability
体内研究(In Vivo)
ODM-203 (20, 40 mg/kg; p.o.; single daily for 21 days) inhibits FGFR phosphorylation and tumor growth in several FGFR-dependent xenografts by suppressing FGFR signaling in tumors.
ODM-203 (7, 20, 40 mg/kg; p.o.; single daily for 21 days) shows strong anti-tumor activity in a VEGFR-dependent angiogenic orthotopic syngenic model (Renca) and suppresses angiogenesis.
ODM-203 (20, 40 mg/kg; p.o.; single daily for 5 days) activates immune response in the tumor microenvironment. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Holmstr?m TH, et al. ODM-203, a Selective Inhibitor of FGFR and VEGFR, Shows Strong Antitumor Activity, and Induces Antitumor Immunity. Mol Cancer Ther. 2019 Jan;18(1):28-38.
溶解度数据
In Vitro: DMSO : 66.67 mg/mL (131.88 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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