2. Protein Tyrosine Kinase/RTK Apoptosis
  3. FGFR Apoptosis
  4. FGFR-IN-8

FGFR-IN-8 (Compound 17a) 一种高效且具有口服活性的 FGFR 抑制剂，可抑制野生型和突变型 FGFR。 FGFR-IN-8 对 FGFR1、V564F-FGFR2、N549H-FGFR2、V555M-FGFR3、FGFR3 和 FGFR 4的 IC50 值分别为 <0.5、189.1、<0.5、22.6、<0.5 和 7.30 nM。FGFR-IN-8 诱导癌细胞凋亡（apoptosis），具有抗癌活性。

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FGFR-IN-8 Chemical Structure

FGFR-IN-8 Chemical Structure

CAS No. : 2640217-64-5

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FGFR-IN-8 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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FGFR-IN-8 (Compound 17a) is a highly potent and orally active panFGFR inhibitor against wild-type and mutant FGFRs. FGFR-IN-8 shows inhibition with IC50 values of <0.5, 189.1, <0.5, 22.6, <0.5 and 7.30 nM against FGFR1, V564F-FGFR2, N549H-FGFR2, V555M-FGFR3, FGFR3 and FGFR4, respectively. GFR-IN-8 induces cancer cell apoptosis and shows anticancer activities[1].

IC50 & Target

FGFR1

<0.5 nM (IC50)

V564F-FGFR2

189.1 nM (IC50)

N549H-FGFR2

<0.5 nM (IC50)

V555M-FGFR3

22.6 nM (IC50)

FGFR3

<0.5 nM (IC50)

FGFR4

7.30 nM (IC50)

V561M-FGFR1

262.5 nM (IC50)

K650E-FGFR3

<0.5 nM (IC50)

K650M-FGFR3

4.8 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
AN3-CA GI50
0.021 μM
Compound: 17a
Antiproliferative activity against human AN3-CA cells harboring FGFR2 K310R/N549K mutant assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against human AN3-CA cells harboring FGFR2 K310R/N549K mutant assessed as cell growth inhibition by CellTiter-Glo assay
[PMID: 35436119]
BaF3 GI50
> 5 μM
Compound: 17a
Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition by CellTiter-Glo assay
[PMID: 35436119]
BaF3 GI50
0.005 μM
Compound: 17a
Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3 assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3 assessed as cell growth inhibition by CellTiter-Glo assay
[PMID: 35436119]
BaF3 GI50
0.183 μM
Compound: 17a
Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3-V555M mutant assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3-V555M mutant assessed as cell growth inhibition by CellTiter-Glo assay
[PMID: 35436119]
BaF3 GI50
0.749 μM
Compound: 17a
Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 V550E mutant assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 V550E mutant assessed as cell growth inhibition by CellTiter-Glo assay
[PMID: 35436119]
BaF3 GI50
1.677 μM
Compound: 17a
Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 N535K mutant assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 N535K mutant assessed as cell growth inhibition by CellTiter-Glo assay
[PMID: 35436119]
J82 GI50
0.547 μM
Compound: 17a
Antiproliferative activity against human J82 cells harboring FGFR3 K652E mutant assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against human J82 cells harboring FGFR3 K652E mutant assessed as cell growth inhibition by CellTiter-Glo assay
[PMID: 35436119]
KMS-11 GI50
0.034 μM
Compound: 17a
Antiproliferative activity against human KMS-11 cells harboring FGFR3 Y373C mutant assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against human KMS-11 cells harboring FGFR3 Y373C mutant assessed as cell growth inhibition by CellTiter-Glo assay
[PMID: 35436119]
分子量

584.50

Formula

C27H31Cl2N9O2
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-8 相关分类

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  • 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-82640217-64-5FGFRApoptosisFibroblast growth factor receptorBa/F3anticancerorally activeInhibitorinhibitorinhibit

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