2. Protein Tyrosine Kinase/RTK
  3. FGFR
  4. FGFR-IN-11

FGFR-IN-11 (compound I-5) 是一种具有口服活性和共价 pan-FGFR 抑制剂，其 IC50 值分别为 9.9 nM (FGFR1)， 3.1 nM (FGFR2)， 16 nM (FGFR3) 和 1.8 nM (FGFR4)。FGFR-IN-11 以纳摩尔级抑制多种肿瘤细胞增殖。FGFR-IN-11 在荷瘤小鼠模型中显著抑制肿瘤生长。

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FGFR-IN-11 Chemical Structure

FGFR-IN-11 Chemical Structure

CAS No. : 2658488-68-5

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FGFR-IN-11 相关抗体

Top Publications Citing Use of Products

查看 FGFR 亚型特异性产品:

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FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FGFR-IN-11 (compound I-5) is an orally active and covalent FGFR inhibitor with IC50 values of 9.9 nM (FGFR1), 3.1 nM (FGFR2), 16 nM (FGFR3), and 1.8 nM (FGFR4), respectively. FGFR-IN-11 inhibits multiple cancer cell proliferation with nanomolar activity. FGFR-IN-11 inhibits tumor growth significantly in xenograft mice models[1].

IC50 & Target[1]

FGFR1

9.9 nM (IC50)

FGFR2

3.1 nM (IC50)

FGFR3

16 nM (IC50)

FGFR4

1.8 nM (IC50)

体外研究
(In Vitro)

FGFR-IN-11 (0.3 nM-20 μM， 72 h) 以纳摩尔活性抑制多种癌细胞生长[1]。

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

FGFR-IN-11 相关抗体:

Cell Viability Assay[1]

Cell Line: NCI-H1581, SNU16, Huh-7, Hep3B
Concentration: 0.3 nM-20 μM
Incubation Time: 72 h
Result: Inhibited cell growth with IC50 values of less than 2 nM (NCI-H1581 and SNU16), 15.63 nM (Huh-7) and 52.6 nM (Hep3B).
体内研究
(In Vivo)

FGFR-IN-11 (60 mg/kg， 口服， 每天一次， 21 天) 在雌性裸鼠的 Huh-7 或 NCI-H1581 异种移植瘤模型中显著抑制肿瘤生长并且不影响小鼠体重。[1]

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

Animal Model: Huh-7 xenograft model in female nude mice[1]
Dosage: 15, 30, 60 mg/kg
Administration: Oral administration (p.o.)
Result: Inhibited tumor growth of 88.2% at the dose of 60 mg/kg and had no significant changes in body weight.
Animal Model: NCI-H1581 xenograft model in female nude mice[1]
Dosage: 60 mg/kg
Administration: Oral administration (p.o.)
Result: Inhibited tumor growth of 67% and had no significant changes in body weight.
分子量

521.01

Formula

C28H29ClN4O4
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

FGFR-IN-11 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
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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.

Keywords:

FGFR-IN-112658488-68-5FGFRFibroblast growth factor receptorNCI-H1581SNU16Huh-7Hep3Borally activitycovalentxenograft mice modelsanticancerInhibitorinhibitorinhibit

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