Referencia número: HY-15813

FIIN-1

(Synonyms: FGFR irreversible inhibitor-1)

Revisión del cliente

Based on 1 Customer Validation

FIIN-1 is a potent, irreversible, selective FGFR inhibitor. FIIN-1 binds to FGFR1/2/3/4 and Flt1/4 with K_ds of 2.8/6.9/5.4/120 nM and 32/120 nM respectively. The biochemical IC₅₀s of FIIN-1 are 9.2, 6.2, 11.9, and 189 nM against FGFR1/2/3/4, respectively.

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Pureza: 99.04%
No. CAS: 1256152-35-8
Fòrmula: C₃₂H₃₉Cl₂N₇O₄
Peso molecular:656.60

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

FIIN-1 Chemical Structure

No. CAS: 1256152-35-8

Tamaño

Precio

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Cantidad

Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target^[1]

FGFR1

2.8 nM (Kd)

FGFR2

6.9 nM (Kd)

FGFR3

5.4 nM (Kd)

FGFR4

120 nM (Kd)

FGFR1

9.2 nM (IC₅₀)

FGFR2

6.2 nM (IC₅₀)

FGFR3

11.9 nM (IC₅₀)

FGFR4

189 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
NCI-H520	IC₅₀	121 nM Compound: 1; FIIN-1	Antiproliferative activity against human FGFR1-amplified NCI-H520 cells after 7 days by SRB assay Antiproliferative activity against human FGFR1-amplified NCI-H520 cells after 7 days by SRB assay	[PMID: 28521156]
SW780	IC₅₀	277 nM Compound: 1; FIIN-1	Antiproliferative activity against human FGFR3-amplified SW780 cells after 5 days by SRB assay Antiproliferative activity against human FGFR3-amplified SW780 cells after 5 days by SRB assay	[PMID: 28521156]

In Vitro

FIIN-1 binds to BLK, ERK5, KIT, MET, PDGFRB and VEGFR2 with K_ds of 65 nM, 160, 420, 1000, 480 and 210 nM, respectively. The IC₅₀s for Blk and Flt1 are 381 nM and 661 nM respectively^[1].
FIIN-1 (14 nM-46 μM; 72 hours) inhibits proliferation of FGF signaling-sensitive cancer cell lines^[1].
FIIN-1 (20 nM) inhibits iFGFR1 autophosphorylation and its downstream Erk1/2 almost completely.

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

Cell Proliferation Assay^[1]

Cell Line:

Stomach KATO III, SNU-16 and FU97 cells; Bladder RT4 cells; Kidney G-401 and G-402 cells; Lung SBC-3 and H520 cells; Pancreas A2.1 cells; Ovary A2780 and PA-1 cells; Bone RD-ES cells
Concentration:
Incubation Time:

72 hours
Result:

The EC₅₀ of 70 nM for Bladder RT4 cell.
The EC₅₀ of 230 nM for Pancreas A2.1 cell.
The EC₅₀ of 2.3 μM for Bone RD-ES cell.
EC₅₀s of 0.22 and 4.6 μM for Ovary A2780 and PA-1 cells, respectively.
EC₅₀s of 0.08 and 4.5 μM for Lung SBC-3 and H520 cells, respectively.
EC₅₀s of 0.14 and 1.65 μM for Kidney G-401 and G-402 cells, respectively.
EC₅₀s of 0.014, 0.03 and 0.65 μM for Stomach KATO III, SNU-16, FU97 cells, respectively.

Western Blot Analysis^[1]

Cell Line:

Serum-starved MCF10A cells that stably express iFGFR1
Concentration:

20 nM
Incubation Time:

30 minutes
Result:

Blocked activation of iFGFR1 and phosphorylation of downstream effectors Erk1/2.

Chemical Information

No. CAS 1256152-35-8
Appearance Solid
Peso molecular 656.60
Fòrmula C₃₂H₃₉Cl₂N₇O₄
Color White to off-white
SMILES

C=CC(NC1=CC=CC(CN(C2=NC(NCCCCN(CC)CC)=NC=C2CN3C4=C(Cl)C(OC)=CC(OC)=C4Cl)C3=O)=C1)=O
Synonyms

FGFR irreversible inhibitor-1
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (152.30 mM; Need ultrasonic; 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

1.5230 mL

7.6150 mL

15.2300 mL

5 mM

0.3046 mL

1.5230 mL

3.0460 mL

10 mM

0.1523 mL

0.7615 mL

1.5230 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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: ≥ 2.08 mg/mL (3.17 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.17 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (275 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Wenjun Zhou, et al. A structure-guided approach to creating covalent FGFR inhibitors. Chem Biol. 2010 Mar 26;17(3):285-95. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.5230 mL	7.6150 mL	15.2300 mL	38.0749 mL
	5 mM	0.3046 mL	1.5230 mL	3.0460 mL	7.6150 mL
	10 mM	0.1523 mL	0.7615 mL	1.5230 mL	3.8075 mL
	15 mM	0.1015 mL	0.5077 mL	1.0153 mL	2.5383 mL
	20 mM	0.0761 mL	0.3807 mL	0.7615 mL	1.9037 mL
	25 mM	0.0609 mL	0.3046 mL	0.6092 mL	1.5230 mL
	30 mM	0.0508 mL	0.2538 mL	0.5077 mL	1.2692 mL
	40 mM	0.0381 mL	0.1904 mL	0.3807 mL	0.9519 mL
	50 mM	0.0305 mL	0.1523 mL	0.3046 mL	0.7615 mL
	60 mM	0.0254 mL	0.1269 mL	0.2538 mL	0.6346 mL
	80 mM	0.0190 mL	0.0952 mL	0.1904 mL	0.4759 mL
	100 mM	0.0152 mL	0.0761 mL	0.1523 mL	0.3807 mL

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FIIN-1

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Covalent Screening Library

Reprogramming Compound Library

Anti-Lung Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Prostate Cancer Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors 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

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

FIIN-1

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Covalent Screening Library

Reprogramming Compound Library

Anti-Lung Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Prostate Cancer Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors 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

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

FIIN-1 Related Classifications

HY-15813 Related Classifications