2. Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease
  3. FGFR VEGFR Bcr-Abl FLT3 Cytochrome P450
  4. FGFRs-IN-1

FGFRs-IN-1 (Compound A16) 是口服有效的 FGFR 抑制剂，可抑制 FGFR1/2/3/4，IC50 分别为 2.3、7、11 和 163 nM。FGFRs-IN-1 还可抑制 VEGFR1/2/3、Abl 和 Flt3，IC50 分别为 61、176、112、26 和 353 nM。FGFRs-IN-1 对 CYP 酶的抑制效果较弱。 FGFRs-IN-1 可降低 α-SMA 和胶原蛋白 I (collagen I) 的表达，并在 TGF-β1 刺激的 A549 细胞中抑制上皮-间质转化 (EMT)。FGFRs-IN-1 在 Bleomycin (HY-17565) 诱导的小鼠肺纤维化模型和 CCl4 (HY-Y0298) 诱导的小鼠肝纤维化模型中表现出抗炎活性。

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FGFRs-IN-1 Chemical Structure

FGFRs-IN-1 Chemical Structure

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Customer Review

FGFRs-IN-1 相关抗体

Top Publications Citing Use of Products

查看 VEGFR 亚型特异性产品:

查看所有亚型
VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

查看 Cytochrome P450 亚型特异性产品:

查看所有亚型
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FGFRs-IN-1 (Compound A16) is the orally active inhibitor for FGFR, that inhibits FGFR1/2/3/4 with IC50s of 2.3, 7, 11, and 163 nM, respectively. FGFRs-IN-1 also inhibits VEGFR1/2/3, Abl, and Flt3 with IC50s of 61, 176, 112, 26, and 353 nM, respectively. FGFRs-IN-1 exhibits weak inhibitory efficacy against CYP enzymes. FGFRs-IN-1 reduces the expression of α-SMA and collagen I, and inhibits epithelial-mesenchymal transition (EMT) in TGF-β1 stimulated A549 cell. FGFRs-IN-1 exhibits anti-inflammatory activity in Bleomycin (HY-17565)-induced mouse pulmonary fibrosis model and CCl4 (HY-Y0298)-induced mouse liver fibrosis model[1].

IC50 & Target

FGFR1

2.3 nM (IC50)

FGFR2

7 nM (IC50)

FGFR3

11 nM (IC50)

Abl

26 nM (IC50)

Flt-1

61 nM (IC50)

Flt-4

112 nM (IC50)

FGFR4

163 nM (IC50)

KDR

176 nM (IC50)

Flt3

353 nM (IC50)

CYP2D6

9.27 μM (IC50)

CYP2C19

11.46 μM (IC50)

CYP1A2

26.33 μM (IC50)

分子量

537.44

Formula

C28H26Cl2N4O3
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

FGFRs-IN-1 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 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

FGFRs-IN-1FGFRVEGFRBcr-AblFLT3Cytochrome P450Fibroblast growth factor receptorVascular endothelial growth factor receptorCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3CYPsorally activepulmonary fibrosisliver fibrosis,anti-fibroticA549Inhibitorinhibitorinhibit

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产品名称：
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目录号：
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