2. Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  3. FGFR PDGFR EGFR Src
  4. PD-089828

PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC50s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC50=0.18 µM). PD-089828 also inhibits MAPK with an IC50 of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity.

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PD-089828 Chemical Structure

PD-089828 Chemical Structure

CAS No. : 179343-17-0

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10 mg USD 150 In-stock
25 mg USD 320 In-stock
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Based on 1 publication(s) in Google Scholar

PD-089828 Related Antibodies

Top Publications Citing Use of Products

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PDGFR PDGFRβ PDGFRα

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

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Lck Fyn Blk

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC50s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC50=0.18 µM). PD-089828 also inhibits MAPK with an IC50 of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity[1].

IC50 & Target[1]

FGFR1

0.15 μM (IC50)

PDGFR-β

1.76 μM (IC50)

EGFR

5.47 μM (IC50)

c-Src

0.18 μM (IC50)

FGFR1

0.14 μM (Ki)

PDGFR-β

2.38 μM (Ki)

EGFR

3.16 μM (Ki)

c-Src

0.1 μM (Ki)

Cellular Effect
Cell Line Type Value Description References
A549 IC50
4.34 μM
Compound: PD089828
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
[PMID: 25736993]
B16-F10 IC50
2.62 μM
Compound: PD089828
Cytotoxicity against mouse B16F10 cells after 72 hrs by MTT assay
Cytotoxicity against mouse B16F10 cells after 72 hrs by MTT assay
[PMID: 25736993]
HeLa 229 IC50
3.87 μM
Compound: PD089828
Cytotoxicity against human HeLa 229 cells after 72 hrs by MTT assay
Cytotoxicity against human HeLa 229 cells after 72 hrs by MTT assay
[PMID: 25736993]
L02 IC50
28.37 μM
Compound: PD089828
Cytotoxicity against human HL7702 cells after 72 hrs by MTT assay
Cytotoxicity against human HL7702 cells after 72 hrs by MTT assay
[PMID: 25736993]
In Vitro

PD-089828 (0.5-20 µM; 2 hours) inhibits PDGFR autophosphorylation with an IC50 of 0.82 µM[1].
PD-089828 (1-50 µM; 2 hours) inhibits EGFR autophosphorylation with an IC50 value of 10.9 µM[1].
In A121(p) cells, PD 089828 potently inhibits the phosphorylation of FGFR-1 with an IC50 value of 0.63 µM[1]. PD-089828 (10 µM; 8 days) produces a concentration-related inhibition of serum-stimulated cell growth with an IC50 value of 1.8 µM[1].
PD-089828 inhibits increases in DNA synthesis stimulated by all three growth factors, with IC50 values of 0.8 for PDGF-, 1.7 for EGF- and 0.48 µM for bFGF-induced mitogenesis[1].

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

PD-089828 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: Vascular smooth muscle cells (serum-stimulated growth)
Concentration: 10 µM
Incubation Time: 8 consecutive days
Result: Produced a concentration-related inhibition of serum-stimulated cell growth with an IC50 value of 1.8 µM.

Western Blot Analysis[1]

Cell Line: Vascular smooth muscle cells (stimulated with PDGF-BB 30 ng/ml)
Concentration: 0.5-20 µM
Incubation Time: 2 hours
Result: Inhibited PDGFR autophosphorylation with an IC50 of 0.82 µM.
Molecular Weight

405.28

Formula

C18H18Cl2N6O
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(NC(C)(C)C)NC1=NC2=NC(N)=NC=C2C=C1C3=C(Cl)C=CC=C3Cl
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 : 10 mg/mL (24.67 mM; ultrasonic and warming and heat to 60°C; 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 2.4674 mL 12.3371 mL 24.6743 mL
5 mM 0.4935 mL 2.4674 mL 4.9349 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
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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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: ≥ 0.56 mg/mL (1.38 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.56 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.6 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: ≥ 0.56 mg/mL (1.38 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.56 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 (5.6 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

Purity: 98.07%

SDS (251 KB)

COA (255 KB) HNMR (257 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
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 2.4674 mL 12.3371 mL 24.6743 mL 61.6857 mL
5 mM 0.4935 mL 2.4674 mL 4.9349 mL 12.3371 mL
10 mM 0.2467 mL 1.2337 mL 2.4674 mL 6.1686 mL
15 mM 0.1645 mL 0.8225 mL 1.6450 mL 4.1124 mL
20 mM 0.1234 mL 0.6169 mL 1.2337 mL 3.0843 mL
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PD-089828 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:

PD-089828179343-17-0PD089828PD 089828FGFRPDGFREGFRSrcFibroblast growth factor receptorPlatelet-derived growth factor receptorEpidermal growth factor receptorErbB-1HER1ATPcompetitiveautophosphorylationphosphorylationvascularsmoothmusclecellsnonselectiveantiproliferativeantimigratoryInhibitorinhibitorinhibit

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