1. Protein Tyrosine Kinase/RTK
  2. FGFR
  3. FGFR1 inhibitor-11

FGFR1 inhibitor-11 (compound 5g) 与 FGFR1 结合,其下游 ERK1/2 和 IκBα/NF-κB 信号传导失活可抑制 RANKL 诱导的破骨细胞生成。FGFR1 inhibitor-11 有口服活性。

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FGFR1 inhibitor-11 Chemical Structure

FGFR1 inhibitor-11 Chemical Structure

CAS No. : 2157482-40-9

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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

FGFR1 inhibitor-11 (compound 5g) binds to FGFR1, inactivation of its downstream ERK1/2 and IκBα/NF-κB signaling inhibited RANKL-induced osteoclastogenesis. FGFR1 inhibitor-11 has oral bioactivity[1].

体外研究
(In Vitro)

FGFR1 inhibitor-11 (compound 5g) (0-20μM,4 天) 可减弱骨髓来源巨噬细胞中 RANKL 诱导的破骨细胞生成[1]
FGFR1 inhibitor-11 (0-160 μM; 48 h) 在低于 20 μM 的 BMDM 中没有表现出明显的毒性[1]
FGFR1 inhibitor-11 (0-10 μM) 抑制 F-肌动蛋白带的形成[1]
FGFR1 inhibitor-11 (0-10 μM) 通过减少 NFATc1 和 c-fos 来抑制破骨细胞生成所需基因的表达,从而抑制破骨细胞生成[1]

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

Cell Viability Assay[1]

Cell Line: BMDMs
Concentration: 0, 1.25 μM, 2.5 μM, 5 μM, 10 μM, 20 μM, 40 μM, 80 μM, 160 μM
Incubation Time: 48 h
Result: Had toxicity in BMDMs above 40 μM.

Immunofluorescence[1]

Cell Line: Osteoclasts
Concentration: 0, 2.5μM, 5 μM, 10 μM
Incubation Time:
Result: Showed significantly and dose dependently the protein level of F-actin.

Real Time qPCR[1]

Cell Line: BMDMs
Concentration: 10 μM
Incubation Time: 1 day, 2 days, 3 days
Result: Showed inhibition of the mRNA expression level (Ctsk, Mmmp9 and so on) of the main osteoclast-specific marker genes.
体内研究
(In Vivo)

FGFR1 inhibitor-11 (15-30 mg/kg; 口服;每天 2 次)可显着预防小鼠骨质流失 (BV、T-BMD 等)[1]

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

分子量

358.39

Formula

C23H18O4

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

FGFR1 inhibitor-11 相关分类

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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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FGFR1 inhibitor-11
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HY-158098
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