1. Protein Tyrosine Kinase/RTK
  2. FGFR
  3. FGFR1 inhibitor-6

FGFR1 inhibitor-6 is a potent FGFR1 inhibitor with an IC50 value of 16.31 nM. FGFR1 inhibitor-6 shows cytotoxic activities. FGFR1 inhibitor-6 induces apoptosis and cell cycle arrest at pre-G1 and G2/M phase.

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FGFR1 inhibitor-6 Chemical Structure

FGFR1 inhibitor-6 Chemical Structure

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Description

FGFR1 inhibitor-6 is a potent FGFR1 inhibitor with an IC50 value of 16.31 nM. FGFR1 inhibitor-6 shows cytotoxic activities. FGFR1 inhibitor-6 induces apoptosis and cell cycle arrest at pre-G1 and G2/M phase[1].

IC50 & Target[1]

FGFR1

16.31 nM (IC50)

In Vitro

FGFR1 inhibitor-6 (compound 3) (48 h) shows cytotoxic activities with IC50s of 2.06, 0.73, 97.2 µM for HepG-2, MCF-7, WI-38 cells, respectively[1].
FGFR1 inhibitor-6 (0.73 µM; 24 h) induces apoptosis and cell cycle arrest at pre-G1 and G2/M phase[1].
FGFR1 inhibitor-6 (0.73 µM; 24 h) increases the expression of caspase-3/7/9 protein levels in MCF-7 cells[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: HepG-2, MCF-7, WI-38 cells
Concentration:
Incubation Time: 48 h
Result: Showed cytotoxic activities with IC50s of 2.06, 0.73, 97.2 µM for HepG-2, MCF-7, WI-38 cells, respectively.

Cell Cycle Analysis[1]

Cell Line: MCF-7 cells
Concentration: 0.73 µM
Incubation Time: 24 h
Result: Induced pronounced increase in the cell percentages at pre-G1 and G2/M phase at 27.72% and 19.22%, respectively.

Apoptosis Analysis[1]

Cell Line: MCF-7 cells
Concentration: 0.73 µM
Incubation Time: 24 h
Result: Induced apoptosis with late apoptosis percentages are 11.24 % and the early apoptosis percentages from 1.59% to 5.07%.

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 0.73 µM
Incubation Time: 24 h
Result: Increased the expression of caspase-3/7/9 protein levels with the caspase-3, aspase-7, aspase-9 protein levels increased to 5.60, 11.62, 7.14 folds, respectively comparing with the untreated cells.
Molecular Weight

541.60

Formula

C27H19N5O4S2

SMILES

COC1=CC(C2=NC3=CC=CC=C3S2)=CC=C1OCC(N/N=C4NC(/C(S/4)=C/C5=CC=C(C=C5)C#N)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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FGFR1 inhibitor-6 Related Classifications

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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.

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Product Name:
FGFR1 inhibitor-6
Cat. No.:
HY-143272
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