2. Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease
  3. FGFR Cytochrome P450
  4. FGFR-IN-10

FGFR-IN-10 是一种口服有效的 FGFR 和 Cytochrome P450 (CYP) 抑制剂。FGFR-IN-10 抑制野生型和 V564F 突变型 FGFR2 的 IC50 分别为 104.1 nM 和 43.6 nM。FGFR-IN-10 还抑制 CYP，IC50 分别为 3.33 μM (CYP2C9)，18.75 μM (CYP2C19)，4.34 μM (CYP2CD6)，和 0.69 μM (CYP3A4)。

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FGFR-IN-10 Chemical Structure

FGFR-IN-10 Chemical Structure

CAS No. : 2847092-41-3

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FGFR-IN-10 相关抗体

Top Publications Citing Use of Products

查看 FGFR 亚型特异性产品:

查看所有亚型
FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

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 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FGFR-IN-10 is an orally active inhibitor of FGFR and Cytochrome P450 (CYPs). FGFR-IN-10 inhibits wide type and V564F mutant FGFR2 with IC50s of 104.1 nM and 43.6 nM, respectively. FGFR-IN-10 also inhibits CYPs with IC50s of 3.33 μM (CYP2C9), 18.75 μM (CYP2C19), 4.34 μM (CYP2CD6), and 0.69 μM (CYP3A4), respectively[1].

IC50 & Target[1]

CYP2C9

3.33 μM (IC50)

CYP2C19

18.75 μM (IC50)

CYP2D6

4.34 μM (IC50)

CYP3A4

0.69 μM (IC50)

FGFR2

104.1 nM (IC50)

V564F-FGFR2

43.6 nM (IC50)

体外研究
(In Vitro)

FGFR-IN-10 (compound 115) (5 μM; 0-240 min) 在 SD 大鼠和人血液中具有稳定性，其全血半衰期均 (t1/2) >600 min[1]。
FGFR-IN-10 (0-10 μM; 72 h) 抑制 SNU-16 和 JMSU-1 细胞的生长，GI50 分别为 6 nM 和 24 nM[1]。

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

FGFR-IN-10 相关抗体:
体内研究
(In Vivo)

FGFR-IN-10 (10 mg/kg; 口服; 单剂量) 在 SD 大鼠中表现出较强的口服活性，生物利用度为 60.7%[1]。

在 SD 大鼠中的药代动力学分析[1]

Route Dose (mg/kg) Cmax (ng/mL) AUClast/D (h·mg/mL) T1/2 (h) Cl_obs (mL/min/kg) Vss_obs (L/kg) F (%)
i.v. 5 / 664 1.02 26.0 1.2 /
p.o. 10 2388 402 / / / 60.7

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

543.60

Formula

C28H30FN9O2
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-10 相关分类

  • 摩尔计算器

  • 稀释计算器

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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-102847092-41-3FGFRCytochrome P450Fibroblast growth factor receptorCYPsInhibitorinhibitorinhibit

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