2. Protein Tyrosine Kinase/RTK
  3. FGFR
  4. FGFR4-IN-8

FGFR4-IN-8 (Compound 7v) 是一种 ATP 竞争性、高度选择性的野生型和突变型 FGFR4 共价抑制剂。FGFR4-IN-8 对 FGFR4、FGFR4V550L、FGFR4V550M 和 FGFR4C552S 的 IC50 分别为 0.5、0.25、1.6、931 nM。FGFR4-IN-8 有效抗 Hep3B 肝细胞癌细胞增殖，IC50 值为

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FGFR4-IN-8 Chemical Structure

FGFR4-IN-8 Chemical Structure

CAS No. : 2765240-52-4

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FGFR4-IN-8 相关抗体

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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

FGFR4-IN-8 (Compound 7v) is an ATP-competitive, highly selective covalent inhibitor of wild-type and gatekeeper mutant FGFR4. FGFR4-IN-8 exhibits excellent potency against FGFR4, FGFR4V550L, FGFR4V550M and FGFR4C552S with IC50s of 0.5, 0.25, 1.6, 931 nM, respectively. FGFR4-IN-8 exhibits potent antiproliferative activity against Hep3B hepatocellular carcinoma cells with the IC50 value of 29 nM. FGFR4-IN-8 demonstrates modest in vivo antitumor efficacy in nude mice bearing the Huh-7 xenograft model[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
BaF3 IC50
> 1 μM
Compound: 7v
Antiproliferative activity against mouse BAF3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BAF3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
[PMID: 35271262]
BaF3 IC50
0.0035 μM
Compound: 7v
Antiproliferative activity against mouse BAF3 cells expressing wild-type FGFR4 assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BAF3 cells expressing wild-type FGFR4 assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
[PMID: 35271262]
BaF3 IC50
4.7 nM
Compound: 7v
Antiproliferative activity against mouse BAF3 cells expressing FGFR4 V550L mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BAF3 cells expressing FGFR4 V550L mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
[PMID: 35271262]
BaF3 IC50
8.1 nM
Compound: 7v
Antiproliferative activity against mouse BAF3 cells expressing FGFR4 V550M mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BAF3 cells expressing FGFR4 V550M mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
[PMID: 35271262]
Hep 3B2 IC50
0.029 μM
Compound: 7v
Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth incubated for 5 days by SRB assay
Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth incubated for 5 days by SRB assay
[PMID: 35271262]
Huh-7 IC50
72 nM
Compound: 7v
Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth incubated for 5 days by SRB assay
Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth incubated for 5 days by SRB assay
[PMID: 35271262]
MDA-MB-453 IC50
0.034 μM
Compound: 7v
Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell growth incubated for 5 days by SRB assay
Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell growth incubated for 5 days by SRB assay
[PMID: 35271262]
NCI-H1299 IC50
2.97 μM
Compound: 7v
Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth incubated for 5 days by SRB assay
Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth incubated for 5 days by SRB assay
[PMID: 35271262]
分子量

654.56

Formula

C32H34Cl2FN7O3
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

FGFR4-IN-8 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.

Keywords:

FGFR4-IN-82765240-52-4FGFRFibroblast growth factor receptorATP-competitivecovalentwild-typegatekeeper mutantFGFR4Hep3B hepatocellular carcinoma cellsHuh-7 xenograftInhibitorinhibitorinhibit

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