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FIIN-2 FGFR inhibitor

Cat.No.S7714

FIIN-2 is an irreversible, pan-FGFR inhibitor with IC50 of 3.09 nM, 4.3 nM, 27 nM and 45.3 nM for FGFR1/2/3/4, respectively.
FIIN-2 FGFR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 634.73

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Quality Control

Batch: S771401 DMSO]69 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.83%
99.83

Solubility

In vitro
Batch:

DMSO : 69 mg/mL (108.7 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 634.73 Formula

C35H38N8O4

Storage (From the date of receipt)
CAS No. 1633044-56-0 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC=C4CN(C(=O)N(C4=N3)CC5=CC=C(C=C5)NC(=O)C=C)C6=CC(=CC(=C6)OC)OC

Mechanism of Action

Targets/IC50/Ki
FGFR1
(Cell-free assay)
3.09 nM
FGFR2
(Cell-free assay)
4.3 nM
FGFR3
(Cell-free assay)
27 nM
FGFR4
(Cell-free assay)
45.3 nM
In vitro
In FGFR1-4 Ba/F3 cells, FIIN-2 inhibits cell proliferation with EC50 in the single- to double-digit nanomolar range. This compound also shows excellent antiproliferative activity in a variety of backgrounds, including cell lines that have gatekeeper mutations in FGFR1 and that are dependent on FGFR4.
Kinase Assay
Biochemical assays
Biochemical assays are performed by a broad-coverage, TR-FRET-based kinase binding assay platform.
In vivo
In a zebrafish developmental model, FIIN-2 causes mild or severe phenotypes to the tail morphogenesis by inhibiting FGFR.
References

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