Cat. No.: HY-112345

PD-089828

Customer Review

Based on 1 Customer Validation

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.

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

Purity: 98.07%
CAS No.: 179343-17-0
Formula: C₁₈H₁₈Cl₂N₆O
Molecular Weight:405.28

Storage:

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

PD-089828 Chemical Structure

CAS No.: 179343-17-0

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Use of MCE Products

Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

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)

All PDGFR Isoforms :

All EGFR Isoforms :

All Src Isoforms :

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.

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.

Chemical Information

CAS No. 179343-17-0
Appearance Solid
Molecular Weight 405.28
Formula C₁₈H₁₈Cl₂N₆O
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)

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

2.4674 mL

12.3371 mL

24.6743 mL

5 mM

0.4935 mL

2.4674 mL

4.9349 mL

10 mM

0.2467 mL

1.2337 mL

2.4674 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.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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: ≥ 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.

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 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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Portuguese - PT (254 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)
Handling Instructions (2659 KB)

References

[1]. Dahring TK, et al. Inhibition of growth factor-mediated tyrosine phosphorylation in vascular smooth muscle by PD 089828, a new synthetic protein tyrosine kinase inhibitor. J Pharmacol Exp Ther. 1997 Jun;281(3):1446-56. [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	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

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All PDGFR Isoforms

All EGFR Isoforms

All Src Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

PD-089828 Related Classifications

Cat. No.: HY-112345