1. Protein Tyrosine Kinase/RTK
  2. FGFR
  3. E7090

E7090 is an orally available, potent, and selective FGFR inhibitor with IC50s of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/FGFR2/FGFR3/FGFR4, respectively.

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

E7090 Chemical Structure

E7090 Chemical Structure

CAS No. : 1622204-21-0

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 1099 In-stock
Solution
10 mM * 1 mL in DMSO USD 1099 In-stock
Solid
1 mg USD 320 In-stock
5 mg USD 850 In-stock
10 mg USD 1450 In-stock
25 mg USD 3000 In-stock
50 mg USD 4850 In-stock
100 mg USD 7600 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

E7090 is an orally available, potent, and selective FGFR inhibitor with IC50s of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/FGFR2/FGFR3/FGFR4, respectively[1].

IC50 & Target[2]

FGFR1

0.71 nM (IC50)

FGFR2

0.50 nM (IC50)

FGFR3

1.2 nM (IC50)

FGFR4

120 nM (IC50)

In Vitro

E7090 inhibits the growth of SNU-16, human gastric cancer cell line harboring FGFR2 amplification with an IC50 value of 3 nM[1].
E7090 inhibits SNU-16 cell proliferation with an IC50 value of 5.7 nM[2].
E7090 inhibits proliferation of human cancer cell lines harboring various types of FGFRs gene abnormalities such as amplification, mutation, or translocation in vitro, which are confirmed by the inhibition of FGFR signaling[1].
E7090 has interaction kinetics with FGFR1 kinases intermediate between those of the two representative inhibitors, and the residence time of E7090 succinate is 19 minutes[1].

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

Western Blot Analysis[1]

Cell Line: SNU-16 cells
Concentration: 0.4-100 nM
Incubation Time: 4 hours
Result: Inhibited FGFR phosphorylation with an IC50 value of 1.2 nM.
Inhibited the phosphorylation of FRS2a, ERK1/2, and AKT, molecules downstream of FGFRs, in a dose-dependent manner.
In Vivo

Pharmacodynamics analysis reveals that E7090 inhibits phosphorylation of FGFRs in SNU-16 xenograft tumors in a dose-dependent manner[1].
E7090 (6.25-50 mg/kg, orally, once daily) treatment prolongs survival in a 4T1 mouse lung metastasis model[2].

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

Animal Model: Mouse xenograft model of SNU-16 human gastric cancer[2]
Dosage: 6.25 to 50 mg/kg
Administration: Orally, once daily for 14 days
Result: Inhibited tumor growth in a dose-dependent manner.
Clinical Trial
Molecular Weight

587.67

Formula

C32H37N5O6

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1C=CC2=C1C=C(OCCOC)C(OC3=CC(NC(C4=CC=C(C5CCN(CCO)CC5)C=C4)=O)=NC=C3)=C2)NC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (170.16 mM; Need ultrasonic; 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 1.7016 mL 8.5082 mL 17.0164 mL
5 mM 0.3403 mL 1.7016 mL 3.4033 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.

  • Molarity Calculator

  • Dilution Calculator

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: ≥ 2.5 mg/mL (4.25 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.

    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: ≥ 2.5 mg/mL (4.25 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.

    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.
Purity & Documentation
References

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 1.7016 mL 8.5082 mL 17.0164 mL 42.5409 mL
5 mM 0.3403 mL 1.7016 mL 3.4033 mL 8.5082 mL
10 mM 0.1702 mL 0.8508 mL 1.7016 mL 4.2541 mL
15 mM 0.1134 mL 0.5672 mL 1.1344 mL 2.8361 mL
20 mM 0.0851 mL 0.4254 mL 0.8508 mL 2.1270 mL
25 mM 0.0681 mL 0.3403 mL 0.6807 mL 1.7016 mL
30 mM 0.0567 mL 0.2836 mL 0.5672 mL 1.4180 mL
40 mM 0.0425 mL 0.2127 mL 0.4254 mL 1.0635 mL
50 mM 0.0340 mL 0.1702 mL 0.3403 mL 0.8508 mL
60 mM 0.0284 mL 0.1418 mL 0.2836 mL 0.7090 mL
80 mM 0.0213 mL 0.1064 mL 0.2127 mL 0.5318 mL
100 mM 0.0170 mL 0.0851 mL 0.1702 mL 0.4254 mL
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E7090 Related Classifications

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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