1. Protein Tyrosine Kinase/RTK
  2. FGFR
  3. FGFR-IN-9

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 FGFR1IC50 分别为 17.1、29.6、30.7、46.7 和 64.3 nM。

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FGFR-IN-9 Chemical Structure

FGFR-IN-9 Chemical Structure

CAS No. : 3024090-08-9

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查看 FGFR 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[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]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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-9 i.v. 1 mg/kg p.o. 10 mg/kg
T1/2 (h) 1.3 2.37
Tmax (h) / 2
Cmax (ng/mL) / 202
AUCmax (h·ng/mL) 175 965
AUCINF (h·ng/mL) 177 1087
MRTinf (h) 1.13 3.87
F (%) / 61.5
VSS (L/kg) 6.37 /
CL (L/h/kg) 5.65 /

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

CAS 号
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.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
FGFR-IN-9
目录号:
HY-152104
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