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FGFR-IN-9
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
FGFR-IN-9图片
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
FGFR-IN-9 (Compound 19) 是一种有效的、可逆的、具有口服活性的FGFR抑制剂,对 FGFR4WT、FGFR3、FGFR4V550L、FGFR2 和 FGFR1 的IC50分别为 17.1、29.6、30.7、46.7 和 64.3 nM。
生物活性

FGFR-IN-9 (Compound 19) is a potent, reversible and orally activeFGFRinhibitor with anIC50of 17.1, 29.6, 30.7, 46.7 and 64.3 nM againstFGFR4WT,FGFR3,FGFR4V550L,FGFR2andFGFR1, respectively[1].

IC50& Target[1]

FGFR4WT

17.1 nM (IC50)

FGFR3

29.6 nM (IC50)

FGFR4V550L

30.7 nM (IC50)

FGFR2

46.7 nM (IC50)

FGFR1

64.3 nM (IC50)

体外研究
(In Vitro)

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[1]
FGFR-IN-9 (0-400 nM; 4 h) 抑制 FGFR 信号通路[1]

Western Blot Analysis[1]

Cell Line:Ba/F3-TEL-FGFR4 cells
Concentration:0, 50, 100, 200 and 400 nM
Incubation Time:4 h
Result:Showed dose-dependent inhibition of the FGFR4 signal cassette, including the phosphorylation of FGFR4 and its downstream effectors FRS2 and PLCγ.
体内研究
(In Vivo)

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[1]
In Vivo Pharmacokinetic Profile Data for FGFR-IN-9 (Compound 19)[1]

FGFR-IN-9i.v. 1 mg/kgp.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[1]
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[1]
Dosage:1 mg/kg and 10 mg/kg
Administration:i.v. and p.o. (Pharmacokinetic Analysis)
Result:Showed good in vivo pharmacokinetic profile.
分子量

492.59

Formula

C25H28N6O3S

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.