Cat. No.: HY-18603

FIIN-3

Customer Review

Based on 1 Customer Validation

FIIN-3 is an irreversible inhibitor of FGFR with an IC₅₀ of 13.1, 21, 31.4, and 35.3 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.

For research use only. We do not sell to patients.

Purity: 99.01%
CAS No.: 1637735-84-2
Formula: C₃₄H₃₆Cl₂N₈O₄
Molecular Weight:691.61

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

FIIN-3 Chemical Structure

CAS No.: 1637735-84-2

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Top Publications Citing

Use of MCE Products

Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

FIIN-3 is an irreversible inhibitor of FGFR with an IC₅₀ of 13.1, 21, 31.4, and 35.3 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.

IC₅₀ & Target^[1]

FGFR1

13.1 nM (IC₅₀)

FGFR2

21 nM (IC₅₀)

FGFR3

31.4 nM (IC₅₀)

FGFR4

35.3 nM (IC₅₀)

All EGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	EC₅₀	1 nM Compound: 22; FIIN-3	Antiproliferative activity against mouse BaF3 cells harboring wild-type FGFR1 assessed as reduction in cell proliferation measured after 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring wild-type FGFR1 assessed as reduction in cell proliferation measured after 72 hrs by MTS assay	[PMID: 34962782]
BaF3	EC₅₀	1 nM Compound: 22; FIIN-3	Antiproliferative activity against mouse BaF3 cells harboring wild-type FGFR2 assessed as reduction in cell proliferation measured after 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring wild-type FGFR2 assessed as reduction in cell proliferation measured after 72 hrs by MTS assay	[PMID: 34962782]
BaF3	EC₅₀	1 nM Compound: 22; FIIN-3	Antiproliferative activity against mouse BaF3 cells harboring wild-type FGFR3 assessed as reduction in cell proliferation measured after 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring wild-type FGFR3 assessed as reduction in cell proliferation measured after 72 hrs by MTS assay	[PMID: 34962782]
BaF3	EC₅₀	1 nM Compound: 22; FIIN-3	Antiproliferative activity against mouse BaF3 cells harboring wild-type FGFR4 assessed as reduction in cell proliferation measured after 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring wild-type FGFR4 assessed as reduction in cell proliferation measured after 72 hrs by MTS assay	[PMID: 34962782]
BaF3	EC₅₀	64 nM Compound: 22; FIIN-3	Antiproliferative activity against mouse BaF3 cells harboring FGFR2 V564M mutant assessed as reduction in cell proliferation measured after 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring FGFR2 V564M mutant assessed as reduction in cell proliferation measured after 72 hrs by MTS assay	[PMID: 34962782]

In Vitro

FIIN-3 potently inhibits both WT FGFRs (EC₅₀ in the 1- to 41-nM range) and the gatekeeper mutant of FGFR2 (EC₅₀ of 64 nM). FIIN-3 also strongly inhibits EGFR, with an EC₅₀ of 43 nM. FIIN-3 shows good potency against gatekeeper mutant V564F; FIIN-3 also is potent against the gatekeeper-plus-1 mutant E565K; FIIN-3 also displays antiproliferative activity (with an EC₅₀ of 135 nM) against Ba/F3 cells transformed by the EGFR vIII fusion protein, which has a WT EGFR kinase domain. FIIN-3 shows even better activity against EGFR mutant L858R (EC₅₀ of 17 nM) and moderate activity, displaying an EC₅₀ of 231 nM, against the EGFR mutant L858R/T790M mutant. In WT FGFR2 Ba/F3 cells, FIIN-3 completely inhibits the FGFR2 autophosphorylation on Tyr656/657 at concentrations as low as 3 nM. In FGFR2 V564M Ba/F3 cells, FIIN-3 is capable of inhibiting the FGFR2 mutant V564M autophosphorylation with partial inhibition at 100 nM and complete inhibition observed at 300 nM^[1].

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

Chemical Information

CAS No. 1637735-84-2
Appearance Solid
Molecular Weight 691.61
Formula C₃₄H₃₆Cl₂N₈O₄
Color White to off-white
SMILES

C=CC(NC1=CC=C(CN(C(NC2=C(Cl)C(OC)=CC(OC)=C2Cl)=O)C3=NC=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=C3)C=C1)=O
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 10 mg/mL (14.46 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.4459 mL

7.2295 mL

14.4590 mL

5 mM

0.2892 mL

1.4459 mL

2.8918 mL

10 mM

0.1446 mL

0.7230 mL

1.4459 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1 mg/mL (1.45 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 1 mg/mL (1.45 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

Cell Assay^[1]

TEL-FGFR2–transformed Ba/F3 cells are seeded in a 96-well plate and are treated with each concentration of FIIN-3. After 72 h the cells are assessed by MTS tetrazolium assay^[1].

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Tan L et al. 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):E4869-77 [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.4459 mL	7.2295 mL	14.4590 mL	36.1475 mL
	5 mM	0.2892 mL	1.4459 mL	2.8918 mL	7.2295 mL
	10 mM	0.1446 mL	0.7230 mL	1.4459 mL	3.6148 mL

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FIIN-3

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Covalent Screening Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cytokine Inhibitors Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

All EGFR Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

FIIN-3 Related Classifications

Cat. No.: HY-18603