产品
编 号：F762930
分子式：C25H28N6O3S
分子量：492.59
分子式：C25H28N6O3S
分子量：492.59
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CAS No: 3024090-08-9
产品详情
生物活性：
FGFR-IN-9 (Compound 19) is a potent, reversible and orally active FGFR inhibitor with an IC50 of 17.1, 29.6, 30.7, 46.7 and 64.3 nM against FGFR4WT, FGFR3, FGFR4V550L, FGFR2 and FGFR1, respectively.
体内研究：
FGFR-IN-9 (Compound 19) (30 and 45 mg/kg; i.g.; daily for 3 weeks) 在 HUH7 异种移植小鼠模型中显示出抗肿瘤活性。In Vivo Pharmacokinetic Profile Data for FGFR-IN-9 (Compound 19) FGFR-IN-9i.v. 1 mg/kg p.o. 10 mg/kg
T1/2 (h)1.32.37
Tmax (h)/2
Cmax (ng/mL)/202
AUCmax (h·ng/mL)175965
AUCINF (h·ng/mL)1771087
MRTinf (h)1.133.87
F (%)/61.5
VSS (L/kg)6.37/
CL (L/h/kg)5.65/
Animal Model:Female BALB/c nude mice, HUH7 xenograft model
Dosage:30 and 45 mg/kg
Administration:Intragastric gavage; daily for 3 weeks
Result:Resulted in significant tumor growth inhibition with a TGI value of 81% and an IR value of 63% at a dose of 45 mg/kg. No significant body weight loss (<5%) was observed.
Animal Model:Male CD-1 mice
Dosage:1 mg/kg and 10 mg/kg
Administration:i.v. and p.o. (Pharmacokinetic Analysis)
Result:Showed good in vivo pharmacokinetic profile.
体外研究：
FGFR-IN-9 (Compound 19) (0-2 mM; 72 h) 抑制 HUH7 细胞，IC50 为 94.7±28.6 nM，抑制 Ba/F3 FGFR4WT 和 Ba/F3 FGFR4V550L 细胞增殖，IC50 分别为 82.5 ± 19.2 nM 和 260.0 ± 50.2 nM。FGFR-IN-9 (0-400 nM; 4 h) 抑制 FGFR 信号通路。
FGFR-IN-9 (Compound 19) is a potent, reversible and orally active FGFR inhibitor with an IC50 of 17.1, 29.6, 30.7, 46.7 and 64.3 nM against FGFR4WT, FGFR3, FGFR4V550L, FGFR2 and FGFR1, respectively.
体内研究：
FGFR-IN-9 (Compound 19) (30 and 45 mg/kg; i.g.; daily for 3 weeks) 在 HUH7 异种移植小鼠模型中显示出抗肿瘤活性。In Vivo Pharmacokinetic Profile Data for FGFR-IN-9 (Compound 19) FGFR-IN-9i.v. 1 mg/kg p.o. 10 mg/kg
T1/2 (h)1.32.37
Tmax (h)/2
Cmax (ng/mL)/202
AUCmax (h·ng/mL)175965
AUCINF (h·ng/mL)1771087
MRTinf (h)1.133.87
F (%)/61.5
VSS (L/kg)6.37/
CL (L/h/kg)5.65/
Animal Model:Female BALB/c nude mice, HUH7 xenograft model
Dosage:30 and 45 mg/kg
Administration:Intragastric gavage; daily for 3 weeks
Result:Resulted in significant tumor growth inhibition with a TGI value of 81% and an IR value of 63% at a dose of 45 mg/kg. No significant body weight loss (<5%) was observed.
Animal Model:Male CD-1 mice
Dosage:1 mg/kg and 10 mg/kg
Administration:i.v. and p.o. (Pharmacokinetic Analysis)
Result:Showed good in vivo pharmacokinetic profile.
体外研究：
FGFR-IN-9 (Compound 19) (0-2 mM; 72 h) 抑制 HUH7 细胞，IC50 为 94.7±28.6 nM，抑制 Ba/F3 FGFR4WT 和 Ba/F3 FGFR4V550L 细胞增殖，IC50 分别为 82.5 ± 19.2 nM 和 260.0 ± 50.2 nM。FGFR-IN-9 (0-400 nM; 4 h) 抑制 FGFR 信号通路。
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