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Chemical Structure| 1633044-56-0 Chemical Structure| 1633044-56-0

Structure of FIIN-2
CAS No.: 1633044-56-0

Chemical Structure| 1633044-56-0

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FIIN-2 is an irreversible inhibitor of FGFR1-4 with IC50 values of 3.1, 4.3, 27, and 45 nM, respectively.

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Product Details of FIIN-2

CAS No. :1633044-56-0
Formula : C35H38N8O4
M.W : 634.73
SMILES Code : C=CC(NC1=CC=C(CN(C2=NC(NC3=CC=C(N4CCN(C)CC4)C=C3)=NC=C2CN5C6=CC(OC)=CC(OC)=C6)C5=O)C=C1)=O
MDL No. :MFCD28386553

Safety of FIIN-2

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of FIIN-2

RTK

Isoform Comparison

Biological Activity

Target
  • FGFR2

    FGFR2, IC50:4.3 nM

  • FGFR3

    FGFR3, IC50:27 nM

  • FGFR4

    FGFR4, IC50:45.3 nM

  • FGFR1

    FGFR1, IC50:3.09 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
H1581 cells 1 µM 6 hours Evaluate the inhibitory effects of UPR1376 on H1581 cell proliferation PMC6443895
LENTI-4 cells 1 µM 1 hour Evaluate the inhibitory effects of UPR1371-UPR1376 on FGFR1 auto-phosphorylation PMC6443895
H1581 cells (FGFR1 V561M mutant) 23.6 nM 96 hours Evaluate the inhibitory effect of FIIN-2 on the proliferation of FGFR1 V561M mutant H1581 cells, showing an EC50 of 23.6 nM PMC4234547
Ba/F3 cells (FGFR2 V564M mutant) 58 nM 72 hours Evaluate the inhibitory effect of FIIN-2 on the proliferation of FGFR2 V564M mutant Ba/F3 cells, showing an EC50 of 58 nM PMC4234547
Ba/F3 cells (FGFR2-dependent) 1 nM 72 hours Evaluate the inhibitory effect of FIIN-2 on the proliferation of FGFR2-dependent Ba/F3 cells, showing an EC50 of 1 nM PMC4234547
Ba/F3 cells (FGFR1-dependent) 4 nM 72 hours Evaluate the inhibitory effect of FIIN-2 on the proliferation of FGFR1-dependent Ba/F3 cells, showing an EC50 of 4 nM PMC4234547
A549/DDP cells 0-20 μmol/L 24 hours FIIN-2 significantly inhibited the proliferation, colony formation, and migration of A549/DDP cells and induced mitochondria-mediated apoptosis. PMC9428205
A549 cells 0-20 μmol/L 24 hours FIIN-2 significantly inhibited the proliferation, colony formation, and migration of A549 cells and induced mitochondria-mediated apoptosis. PMC9428205
PF179T CAFs 0.3 μM–10 μM 72 hours Test the growth inhibitory effect of FIIN-2 on PF179T CAFs, results showed significant impact on cell viability at 10 μM concentration PMC11413502
CWR-R1 0.3 μM–10 μM 72 hours Test the growth inhibitory effect of FIIN-2 on CWR-R1 cells, results showed effective growth inhibition at approximately 3 μM concentration PMC11413502
VCaP 0.3 μM–10 μM 72 hours Test the growth inhibitory effect of FIIN-2 on VCaP cells, results showed approximately 70% inhibition at 3 μM concentration PMC11413502
LNCaP 0.3 μM–10 μM 72 hours Test the growth inhibitory effect of FIIN-2 on LNCaP cells, results showed cytotoxicity at the highest concentration (10 μM) PMC11413502
Mouse ovarian cells 0.25 μM 5 days To investigate the inhibitory effect of FIIN-2 on FGFRs and its impact on oocyte numbers. Results showed that inhibition of FGFRs led to a decrease in oocyte numbers and upregulated apoptosis levels in the ovaries. PMC10240423

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice (BALB/c) A549/DDP xenograft model Intraperitoneal injection 20 mg/kg Twice daily for 28 days FIIN-2 significantly suppressed tumor growth, and its cytotoxicity was enhanced when combined with the autophagy inhibitor CQ. PMC9428205

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.58mL

0.32mL

0.16mL

7.88mL

1.58mL

0.79mL

15.75mL

3.15mL

1.58mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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