2. Protein Tyrosine Kinase/RTK
  3. FGFR
  4. ASP5878

ASP5878 is an oral active inhibitor of FGFR 1, 2, 3, and 4, with IC50 values of 0.47 nM, 0.6 nM, 0.74 nM and 3.5 nM for FGFR 1, 2, 3, and 4 kinase activity. ASP5878 has potential antineoplastic activity.

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

ASP5878 Chemical Structure

ASP5878 Chemical Structure

CAS No. : 1453208-66-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 220 In-stock
Solution
10 mM * 1 mL in DMSO USD 220 In-stock
Solid
1 mg USD 75 In-stock
5 mg USD 200 In-stock
10 mg USD 300 In-stock
25 mg USD 540 In-stock
50 mg USD 756 In-stock
100 mg USD 1058 In-stock
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Based on 1 publication(s) in Google Scholar

ASP5878 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

ASP5878 is an oral active inhibitor of FGFR 1, 2, 3, and 4, with IC50 values of 0.47 nM, 0.6 nM, 0.74 nM and 3.5 nM for FGFR 1, 2, 3, and 4 kinase activity. ASP5878 has potential antineoplastic activity[1].

IC50 & Target

FGFR1

0.47 nM (IC50)

FGFR2

0.6 nM (IC50)

FGFR3

0.74 nM (IC50)

FGFR4

3.5 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
NIH3T3 IC50
11 nM
Compound: 27
Cytotoxicity against mouse NIH/3T3 cells overexpressing FGFR3 S249C assessed as cell growth inhibition incubated for 5 days by CellTitre-Glo assay
Cytotoxicity against mouse NIH/3T3 cells overexpressing FGFR3 S249C assessed as cell growth inhibition incubated for 5 days by CellTitre-Glo assay
[PMID: 35219181]
In Vitro

ASP5878 shows potent antiproliferative activity in most human HCC cell lines[1].
ASP5878 inhibits FGFR4 phosphorylation in a concentration-dependent manner. ASP5878 treatment results in the suppression of phosphorylation, mobility shift of FRS2, and suppression of ERK phosphorylation[1].

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

ASP5878 Related Antibodies

Cell Viability Assay[1]

Cell Line: Human HCC cell lines.
Concentration: 0-1000 nM.
Incubation Time: 5 days.
Result: HuH-7, Hep3B2.1-7, and JHH-7 cell lines exhibited potent sensitivity to ASP5878, with IC50 values of 27, 8.5, and 21 nmol/L, respectively.
The growth inhibition rate of HLF was 64% and those of other ASP5878-sensitive cell lines were higher than 95% at 1000 nM.
In Vivo

ASP5878 (3 mg/kg, orally, once daily) shows antitumor activity in a Hep3B2.1-7 subcutaneous xenograft and HCC orthotopic xenograft mouse model[1].
ASP5878 induces shrinkage of FGF19-expressing HCC xenograft model[1].

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

Animal Model: Four-week-old male nude mice (CAnN.Cg-Foxn1nu/CrlCrlj [nu/nu]) (Hep3B2.1-7 cells inoculated subcutaneously)[1].
Dosage: 3 mg/kg.
Administration: Orally once daily from days 14 to 52.
Result: Induced tumor regression by 9% and 88% at 1 and 3 mg/kg, respectively, without affecting the body weight for 14 days.
Induced the suppression of FGFR4 phosphorylation, mobility shift of FRS2, and suppression of ERK phosphorylation.
Animal Model: HCC orthotopic xenograft model (mouse)[1].
Dosage: 3 mg/kg.
Administration: Orally once daily for 24 days.
Result: Exhibited a lower tumor burden than vehicle- and sorafenibtreated mice.
Induced sustained tumor regression without tumor regrowth.
Clinical Trial
Molecular Weight

407.37

Formula

C18H19F2N5O4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

OCCN1N=CC(NC2=NC=C(OCC3=C(F)C(OC)=CC(OC)=C3F)C=N2)=C1
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 : ≥ 250 mg/mL (613.69 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4548 mL 12.2739 mL 24.5477 mL
5 mM 0.4910 mL 2.4548 mL 4.9095 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, 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

  • Dilution Calculator

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

Mass
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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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: ≥ 2.08 mg/mL (5.11 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.

    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% Corn Oil

    Solubility: ≥ 2.08 mg/mL (5.11 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

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, 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 2.4548 mL 12.2739 mL 24.5477 mL 61.3693 mL
5 mM 0.4910 mL 2.4548 mL 4.9095 mL 12.2739 mL
10 mM 0.2455 mL 1.2274 mL 2.4548 mL 6.1369 mL
15 mM 0.1637 mL 0.8183 mL 1.6365 mL 4.0913 mL
20 mM 0.1227 mL 0.6137 mL 1.2274 mL 3.0685 mL
25 mM 0.0982 mL 0.4910 mL 0.9819 mL 2.4548 mL
30 mM 0.0818 mL 0.4091 mL 0.8183 mL 2.0456 mL
40 mM 0.0614 mL 0.3068 mL 0.6137 mL 1.5342 mL
50 mM 0.0491 mL 0.2455 mL 0.4910 mL 1.2274 mL
60 mM 0.0409 mL 0.2046 mL 0.4091 mL 1.0228 mL
80 mM 0.0307 mL 0.1534 mL 0.3068 mL 0.7671 mL
100 mM 0.0245 mL 0.1227 mL 0.2455 mL 0.6137 mL
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ASP5878 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.

Keywords:

ASP58781453208-66-6ASP 5878ASP-5878FGFRFibroblast growth factor receptorInhibitorinhibitorinhibit

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