PD-089828
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.
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- Pureza: 98.07%
- No. CAS: 179343-17-0
- Fòrmula: C18H18Cl2N6O
- Peso molecular:405.28
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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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) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
4.34 μM
Compound: PD089828
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Cytotoxicity against human A549 cells after 72 hrs by MTT assay
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
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[PMID: 25736993] |
| B16-F10 | IC50 |
2.62 μM
Compound: PD089828
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Cytotoxicity against mouse B16F10 cells after 72 hrs by MTT assay
Cytotoxicity against mouse B16F10 cells after 72 hrs by MTT assay
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[PMID: 25736993] |
| HeLa 229 | IC50 |
3.87 μM
Compound: PD089828
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Cytotoxicity against human HeLa 229 cells after 72 hrs by MTT assay
Cytotoxicity against human HeLa 229 cells after 72 hrs by MTT assay
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[PMID: 25736993] |
| L02 | IC50 |
28.37 μM
Compound: PD089828
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Cytotoxicity against human HL7702 cells after 72 hrs by MTT assay
Cytotoxicity against human HL7702 cells after 72 hrs by MTT assay
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[PMID: 25736993] |
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.
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Cell Line:Vascular smooth muscle cells (serum-stimulated growth)
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Concentration:10 µM
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Incubation Time:8 consecutive days
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Result:Produced a concentration-related inhibition of serum-stimulated cell growth with an IC50 value of 1.8 µM.
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Cell Line:Vascular smooth muscle cells (stimulated with PDGF-BB 30 ng/ml)
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Concentration:0.5-20 µM
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Incubation Time:2 hours
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Result:Inhibited PDGFR autophosphorylation with an IC50 of 0.82 µM.
Chemical Information
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No. CAS 179343-17-0
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Appearance Solid
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Peso molecular 405.28
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Fòrmula C18H18Cl2N6O
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Color White to light yellow
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SMILES
O=C(NC(C)(C)C)NC1=NC2=NC(N)=NC=C2C=C1C3=C(Cl)C=CC=C3Cl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Ficha de datos (279 KB)
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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)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
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 | 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 |
PD-089828 Related Classifications
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