Art. -Nr.: HY-18602

FIIN-2

Name: FIIN-2
Brand: MedChemExpress
SKU: HY-18602
Price: 58.00 USD
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FIIN-2 is an irreversible inhibitor of FGFR with an IC₅₀ of 3.1, 4.3, 27, and 45 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.

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Reinheit : 99.32%
CAS. Nr.: 1633044-56-0
Formel: C₃₅H₃₈N₈O₄
Molecular Weight:634.73

Speicherung:

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

FIIN-2 Chemical Structure

CAS. Nr.: 1633044-56-0

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

FIIN-2 is an irreversible inhibitor of FGFR with an IC₅₀ of 3.1, 4.3, 27, and 45 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.

IC₅₀ & Target

^[1]

FGFR1

3.1 nM (IC₅₀)

FGFR2

4.3 nM (IC₅₀)

FGFR3

27 nM (IC₅₀)

FGFR4

45 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	EC₅₀	1 nM Compound: 21; FIIN-2	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: 21; FIIN-2	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: 21; FIIN-2	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: 21; FIIN-2	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	58 nM Compound: 21; FIIN-2	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-2 potently inhibits WT FGFRs (EC₅₀s in the 1- to 93-nM range) and the gatekeeper mutant of FGFR2 (EC₅₀ of 58 nM). FIIN-2 also moderately inhibits EGFR, with an IC₅₀ of 204 nM. FIIN-2 inhibits proliferation of FGFR1-4 Ba/F3 cells with EC₅₀s in the single- to double-digit nanomolar range and are especially potent against FGFR2, with EC₅₀s in the 1-nM range. FIIN-2 shows good potency against gatekeeper mutant V564F^[1].

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

In Vivo

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^[1].

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

Chemical Information

CAS. Nr. 1633044-56-0
Appearance Solid
Molecular Weight 634.73
Formel C₃₅H₃₈N₈O₄
Color White to off-white
SMILES

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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (157.55 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

1.5755 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

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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: ≥ 2.5 mg/mL (3.94 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (3.94 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (3.94 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, 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

Protokoll

Cell Assay^[1]

TEL-FGFR2–transformed Ba/F3 cells are seeded in a 96-well plate and are treated with each concentration of the compounds. 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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 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)

Verweise

[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):E4869-4877. [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	1.5755 mL	7.8774 mL	15.7547 mL	39.3868 mL
	5 mM	0.3151 mL	1.5755 mL	3.1509 mL	7.8774 mL
	10 mM	0.1575 mL	0.7877 mL	1.5755 mL	3.9387 mL
	15 mM	0.1050 mL	0.5252 mL	1.0503 mL	2.6258 mL
	20 mM	0.0788 mL	0.3939 mL	0.7877 mL	1.9693 mL
	25 mM	0.0630 mL	0.3151 mL	0.6302 mL	1.5755 mL
	30 mM	0.0525 mL	0.2626 mL	0.5252 mL	1.3129 mL
	40 mM	0.0394 mL	0.1969 mL	0.3939 mL	0.9847 mL
	50 mM	0.0315 mL	0.1575 mL	0.3151 mL	0.7877 mL
	60 mM	0.0263 mL	0.1313 mL	0.2626 mL	0.6564 mL
	80 mM	0.0197 mL	0.0985 mL	0.1969 mL	0.4923 mL
	100 mM	0.0158 mL	0.0788 mL	0.1575 mL	0.3939 mL

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FIIN-2