1. Protein Tyrosine Kinase/RTK
  2. FGFR
  3. FGFR1 inhibitor-10

FGFR1 inhibitor-10 (Compound 4i) is an FGFR1 inhibitor (IC50: 28 nM). FGFR1 inhibitor-10 inhibits the phosphorylation of FGFR1. FGFR1 inhibitor-10 has anti-angiogenic, anti-invasion activity, and anti-tumor effect.

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FGFR1 inhibitor-10

FGFR1 inhibitor-10 Estructura química

No. CAS : 2426769-76-6

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5 mg En stock
10 mg En stock
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100 mg En stock
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500 mg   Obtener un presupuesto  

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Descripciòn

FGFR1 inhibitor-10 (Compound 4i) is an FGFR1 inhibitor (IC50: 28 nM). FGFR1 inhibitor-10 inhibits the phosphorylation of FGFR1. FGFR1 inhibitor-10 has anti-angiogenic, anti-invasion activity, and anti-tumor effect[1].

IC50 & Target

FGFR1

 

Cellular Effect
Cell Line Type Value Description References
U-87MG ATCC IC50
0.12 μM
Compound: 4i
Inhibition of colony formation in human U-87MG cells
Inhibition of colony formation in human U-87MG cells
[PMID: 37651879]
U-87MG ATCC IC50
2.38 μM
Compound: 4i
Antiproliferative activity against human U-87 MG cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human U-87 MG cells incubated for 48 hrs by MTT assay
[PMID: 37651879]
Peso molecular

561.62

Fòrmula

C26H30F3N7O2S

No. CAS
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=C(NC2=NC(NC3=CC=C(N4CCC(N5CCOCC5)CC4)C=C3)=NC=C2C(F)(F)F)SC=C1)NC

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 : 14.29 mg/mL (25.44 mM; ultrasonic and adjust pH to 2 with 1 M HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7806 mL 8.9028 mL 17.8056 mL
5 mM 0.3561 mL 1.7806 mL 3.5611 mL
View the Complete Stock Solution Preparation Table

* 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

  • Calculadora de dilución

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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: 1.43 mg/mL (2.55 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 1.43 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: 1.43 mg/mL (2.55 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 1.43 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
Referencias

Complete Stock Solution Preparation Table

* 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7806 mL 8.9028 mL 17.8056 mL 44.5141 mL
5 mM 0.3561 mL 1.7806 mL 3.5611 mL 8.9028 mL
10 mM 0.1781 mL 0.8903 mL 1.7806 mL 4.4514 mL
15 mM 0.1187 mL 0.5935 mL 1.1870 mL 2.9676 mL
20 mM 0.0890 mL 0.4451 mL 0.8903 mL 2.2257 mL
25 mM 0.0712 mL 0.3561 mL 0.7122 mL 1.7806 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

Nombre del producto:
FGFR1 inhibitor-10
Cat. No.:
HY-156019
Cantidad:
MCE Japan Authorized Agent: