产品
编 号：F161135
分子式：C26H21F2N5O2S
分子量：505.54
分子式：C26H21F2N5O2S
分子量：505.54
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1430723-35-5
产品详情
生物活性：
ODM-203 is an orally active and selective FGFR/VEGFR inhibitor with IC50 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.
体内研究：
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.Animal Model:Athymic Nude-Foxn1nu female mice (9-week-old; subcutaneous xenograft models).
Dosage:20, 40 mg/kg
Administration:Oral administration; single daily for 21 days.
Result:Significantly inhibited tumour growth for 21 consecutive days.Showed tumor growth inhibition (TGI) in RT4 xenografts was 37% and 92% with dosage of 20 and 40 mg/kg, respectively.
Animal Model:Male balb/c mice (8-week-old; orthotopic renca syngenic model).
Dosage:7, 20, 40 mg/kg
Administration:Oral administration; single daily for 21 days.
Result:Showed tumor growth inhibition were 39%, 58% and 75% for dosage of 7, 20 and 40 mg/kg, respectively.Inhibited formation of lung metastasis, and suppressed angiogenesis.
Animal Model:Male balb/c male mice (5 to 7-week-old; renca subcutaneous tumor model).
Dosage:20, 40 mg/kg
Administration:Oral administration; single daily for 5 days.
Result:Resulted in an increase in the percentage of total and CD4 T cells.Decreased the expression of immune check points PD-1 and PD-L1 and increased IFN-γ expression on both CD8 T cells and NK cells.
体外研究：
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.
ODM-203 is an orally active and selective FGFR/VEGFR inhibitor with IC50 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.
体内研究：
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.Animal Model:Athymic Nude-Foxn1nu female mice (9-week-old; subcutaneous xenograft models).
Dosage:20, 40 mg/kg
Administration:Oral administration; single daily for 21 days.
Result:Significantly inhibited tumour growth for 21 consecutive days.Showed tumor growth inhibition (TGI) in RT4 xenografts was 37% and 92% with dosage of 20 and 40 mg/kg, respectively.
Animal Model:Male balb/c mice (8-week-old; orthotopic renca syngenic model).
Dosage:7, 20, 40 mg/kg
Administration:Oral administration; single daily for 21 days.
Result:Showed tumor growth inhibition were 39%, 58% and 75% for dosage of 7, 20 and 40 mg/kg, respectively.Inhibited formation of lung metastasis, and suppressed angiogenesis.
Animal Model:Male balb/c male mice (5 to 7-week-old; renca subcutaneous tumor model).
Dosage:20, 40 mg/kg
Administration:Oral administration; single daily for 5 days.
Result:Resulted in an increase in the percentage of total and CD4 T cells.Decreased the expression of immune check points PD-1 and PD-L1 and increased IFN-γ expression on both CD8 T cells and NK cells.
体外研究：
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.
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