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  1. Protein Tyrosine Kinase/RTK
  2. FGFR
  3. Fisogatinib

Fisogatinib (BLU-554) 是一種有效的高選擇性口服的 FGFR4 抑制劑,其 IC50 值為 5 nM。Fisogatinib 在依賴 FGFR4 信號傳導(dǎo)的肝細(xì)胞癌 (HCC) 模型中具有顯著的抗腫瘤活性。

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Fisogatinib

Fisogatinib Chemical Structure

CAS No. : 1707289-21-1

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10 mM * 1 mL in DMSO ¥1384
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1 mg ¥568
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5 mg ¥1250
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10 mg ¥2000
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Customer Review

Other Forms of Fisogatinib:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Fisogatinib (BLU-554) is a potent, highly selective and orally active fibroblast growth factor receptor 4 (FGFR4) inhibitor with an IC50 of 5 nM. Fisogatinib has significant anti-tumor activity in models of hepatocellular carcinoma (HCC) that are dependent on FGFR4 signalling[1][2].

IC50 & Target[1]

FGFR4

5 nM (IC50)

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
BaF3 IC50
0.396 μM
Compound: BLU-554
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-FGFR4-V550L mutant measured after 24 to 48 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-FGFR4-V550L mutant measured after 24 to 48 hrs by MTT assay
[PMID: 37437349]
BaF3 IC50
0.528 μM
Compound: BLU-554
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-FGFR4-N535K mutant measured after 24 to 48 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-FGFR4-N535K mutant measured after 24 to 48 hrs by MTT assay
[PMID: 37437349]
BaF3 IC50
66.5 nM
Compound: BLU-554
Antiproliferative activity against mouse BaF3 cells expressing TEL-FGFR4 assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BaF3 cells expressing TEL-FGFR4 assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
[PMID: 35635004]
BaF3 IC50
9.2 nM
Compound: 1; BLU554
Antiproliferative activity against mouse BaF3 cells harboring wild type FGFR4 assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BaF3 cells harboring wild type FGFR4 assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 38348819]
BaF3 IC50
> 2000 nM
Compound: 1; BLU554
Antiproliferative activity against mouse BaF3 cells harboring FGFR4 V550L mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BaF3 cells harboring FGFR4 V550L mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 38348819]
BaF3 IC50
> 2000 nM
Compound: 1; BLU554
Antiproliferative activity against mouse BaF3 cells harboring FGFR4 V550M mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BaF3 cells harboring FGFR4 V550M mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 38348819]
Hep 3B2 IC50
0.046 μM
Compound: BLU-554
Antiproliferative activity against human Hep3B cells measured after 24 to 48 hrs by MTT assay
Antiproliferative activity against human Hep3B cells measured after 24 to 48 hrs by MTT assay
[PMID: 37437349]
Hep 3B2 IC50
122 nM
Compound: 8
Antiproliferative activity against FGF19 amplified human Hep3B cells assessed as inhibition of cell growth by SRB assay
Antiproliferative activity against FGF19 amplified human Hep3B cells assessed as inhibition of cell growth by SRB assay
[PMID: 38706130]
Hep 3B2 IC50
40 nM
Compound: BLU-554
Antiproliferative activity against human Hep3B cells expressing FGF19/FGFR4 assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human Hep3B cells expressing FGF19/FGFR4 assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 35635004]
HepG2 IC50
4.431 μM
Compound: BLU-554
Antiproliferative activity against human HepG2 cells measured after 24 to 48 hrs by MTT assay
Antiproliferative activity against human HepG2 cells measured after 24 to 48 hrs by MTT assay
[PMID: 37437349]
Huh-7 IC50
45.9 nM
Compound: 4
Cytotoxicity against human Huh-7 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay
Cytotoxicity against human Huh-7 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay
[PMID: 36480917]
Huh-7 IC50
50 nM
Compound: BLU-554
Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 35635004]
Huh-7 IC50
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