FIIN-2

Alias: FIIN 2; FIIN2; FIIN-2

Cat No.:V0615 Purity: ≥98%

COA Product Data Instructions for use SDS

FIIN-2 (FIIN 2; FIIN2) is a novel irreversible/covalent pan-FGFR inhibitor with potential anticancer activity.

FIIN-2 Chemical Structure CAS No.: 1633044-56-0
Product category: FGFR

This product is for research use only, not for human use. We do not sell to patients.

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Citations by Top Journals: Nature, Cell, Science, etc.

Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

NMR

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Biological Data

Product Description

FIIN-2 (FIIN 2; FIIN2) is a novel irreversible/covalent pan-FGFR inhibitor with potential anticancer activity. It has IC50 values of 3.09 nM, 4.3 nM, 27 nM, and 45.3 nM, which indicate that it inhibits FGFR1/2/3/4. High anti-proliferative activity of FIIN-2 is seen in vitro against cells that are dependent on FGFR1 or FGFR2 gatekeeper mutants.

Biological Activity I Assay Protocols (From Reference)

Targets

FGFR1 (IC50 = 3.1 nM); FGFR2 (IC50 = 4.3 nM); FGFR3 (IC50 = 27 nM); FGFR4 (IC50 = 45 nM)

ln Vitro

FIIN-2 has a potent inhibitory effect on both the gatekeeper mutant of FGFR2 (EC50 of 58 nM) and WT FGFRs (EC50s in the 1- to 93-nM range). With an IC50 of 204 nM, FIIN-2 also moderately inhibits EGFR. FIIN-2 is particularly effective against FGFR2, with EC50s in the 1-nM range, and inhibits the proliferation of FGFR1-4 Ba/F3 cells with EC50s in the single- to double-digit nanomolar range. When it comes to the gatekeeper mutant V564F, FIIN-2 exhibits good potency[1].

ln Vivo

Fish treated in the embryonic stage with FIIN-2 or other known FGFR inhibitors exhibit defects in the posterior mesoderm that are comparable to the phenotypes observed after FGFR is genetically knocked down. In all treated embryonic zebrafish, FIIN-2 results in tail morphogenesis phenotypes that range from mild to severe[1].

Enzyme Assay

A broad-coverage kinase binding assay platform based on TR-FRET is used to conduct biochemical experiments.

Cell Assay

One day after being plated at a density of 1,500 cells per well in 96-well plates, NCI-H2077, NCI-H1581, H520, Kato III, AN3CA, RT112, A2780, 4T1, and SKOV-3 cells are treated with inhibitors. FGFR1 V561M is ectopically overexpressed in NCI-H2077 or NCI-H1581 cells through lentiviral transduction to create the gatekeeper mutation cell lines. Using the Cell-Titer-Glo reagent and the manufacturer's instructions, cell survival is measured 96 hours after the inhibitor is added. GraphPad Prism 5 is used to compute EC50 values. FGF or EGF ligand is also applied to SKOV-3 cells during treatment. A luminometer was used to measure proliferation after 96 hours. Relative values are used to display data. Comparing the luminescence of cells treated with the indicated inhibitor dose to untreated cells is done.

Animal Protocol

Treatment of fish in the embryonic state with either FIIN-2 causes defects to the posterior mesoderm similar to the phenotypes reported following genetic knockdown of FGFR or treatment with other reported FGFR inhibitors. FIIN-2 causes mild or severe phenotypes to the tail morphogenesis in all treated embryonic zebrafish.

zebrafish

References

[1]. Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors. Proc Natl Acad Sci U S A. 2014 Nov 11;111(45):E4869-4877.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

C35H38N8O4

Molecular Weight

634.73

Exact Mass

634.30

Elemental Analysis

C, 66.23; H, 6.03; N, 17.65; O, 10.08

CAS #

1633044-56-0

Related CAS #

1633044-56-0

Appearance

Solid powder

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

InChi Key

DVBPRWJMHURKHP-UHFFFAOYSA-N

InChi Code

InChI=1S/C35H38N8O4/c1-5-32(44)37-26-8-6-24(7-9-26)22-43-33-25(23-42(35(43)45)29-18-30(46-3)20-31(19-29)47-4)21-36-34(39-33)38-27-10-12-28(13-11-27)41-16-14-40(2)15-17-41/h5-13,18-21H,1,14-17,22-23H2,2-4H3,(H,37,44)(H,36,38,39)

Chemical Name

N-[4-[[3-(3,5-dimethoxyphenyl)-7-[4-(4-methylpiperazin-1-yl)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-1-yl]methyl]phenyl]prop-2-enamide

Synonyms

FIIN 2; FIIN2; FIIN-2

HS Tariff Code

2934.99.9001

Storage

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: ~69 mg/mL (~108.7 mM)

Water: <1 mg/mL

Ethanol: <1 mg/mL

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.5755 mL	7.8774 mL	15.7547 mL
	5 mM	0.3151 mL	1.5755 mL	3.1509 mL
	10 mM	0.1575 mL	0.7877 mL	1.5755 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
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See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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Concentration (End)

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
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The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

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Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Biological Data

FIIN-2

Inhibition of FGFR-dependent signaling by BGJ398, FIIN-2, and FIIN-3 in Tel/FGFR2 V564M Ba/F3 cells. Cells were treated with a dose escalation of inhibitors for 6 h and then were lysed and subjected to Western blot for the indicated proteins or phosphoproteins. Proc Natl Acad Sci U S A. 2014 Nov 11; 111(45): E4869–E4877.

Inhibition of FGFR-dependent signaling by BGJ398, FIIN-2, and FIIN-3 in H1581 (FGFR1 WT or V561M) cells. Proc Natl Acad Sci U S A. 2014 Nov 11;111(45):E4869-77.
Effects of FIIN-2, FIIN-3, and FRIN-3 on FGF- and EGF-induced dispersion of SKOV-3 cells in a 3D microfluidic device. Proc Natl Acad Sci U S A. 2014 Nov 11;111(45):E4869-77.