PDGFR-IN-1
Based on 1 Customer Validation
PDGFR-IN-1 (compound 7m) is a potent and orally active PDGFR (platelet-derived growth factor receptor) inhibitor, with IC50 values of 2.4 and 0.9 nM for PDGFRα and PDGFRβ, respectively. PDGFR-IN-1 displays robust antitumor effects and low toxicity, and can be used to study osteosarcoma.
For research use only. We do not sell to patients.
- Purity: 98.84%
- CAS No.: 2644673-07-2
- Formula: C25H30N8O
- Molecular Weight:458.56
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Storage: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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
IC50: 2.4 nM (PDGFRα), 0.9 nM (PDGFRβ)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HOS-TE85 | IC50 |
1.03 μM
Compound: 7m
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Antiproliferative activity against human MNNG/HOS cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human MNNG/HOS cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 35239349] |
| MG-63 | IC50 |
0.44 μM
Compound: 7m
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Antiproliferative activity against human MG-63 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human MG-63 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 35239349] |
| SAOS-2 | IC50 |
0.37 μM
Compound: 7m
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Antiproliferative activity against human SAOS-2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human SAOS-2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 35239349] |
| U2OS | IC50 |
0.42 μM
Compound: 7m
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Antiproliferative activity against human U2OS cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human U2OS cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 35239349] |
PDGFR-IN-1 (compound 7m) (0-0.4 μM, 48 h) inhibits osteosarcoma cancer cells (U2OS, MG63, MNNG/HOS, and SAOS-2) proliferation and colony formation[1].
PDGFR-IN-1 (0-0.4 μM, 48 h) induces cell-cycle arrest in a dose-dependent manner[1].
PDGFR-IN-1 (0-1.6 μM, 48 h) induces MNNG/HOS and MG63 cell apoptosis in a dose-dependent manner[1].
PDGFR-IN-1 (0-0.4 μM, 15 min) inhibits the expression of α-tubulin in both MNNG/HOS and MG63 cells[1].
PDGFR-IN-1 (0-0.4 μM, 48 h) inhibits PDGFRβ phosphorylation and downstream signaling transduction (p-STAT3, p-AKT, and p-ERK)[1].
PDGFR-IN-1 (0-0.4 μM, 48 h) significantly inhibits osteosarcoma cancer cell migration and invasion by downregulating the expression of FAK, as well as the distribution in the leading edge of cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human osteosarcoma cancer cell lines (U2OS, MG63, MNNG/HOS, and SAOS-2)[1]
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Concentration:0.1, 0.2, and 0.4 μM.
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Incubation Time:48 h
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Result:Showed strong antiproliferative activity against MG63, U2OS, MNNG/HOS, and SAOS-2, with IC50 values of 0.44, 0.42, 1.03, and 0.37 μM, respectively. Showed dose-dependent inhibition colony formation.
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Cell Line:MG63 and MNNG/HOS cells[1]
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Concentration:0, 0.1, 0.2, 0.4 μM
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Incubation Time:48 h
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Result:Induced G2/M cell-cycle arrest in MNNG/HOS and G0/G1 cell-cycle arrest in MG63 cells in a dose-dependent manner.
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Cell Line:MG63 and MNNG/HOS cells[1]
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Concentration:0, 0.4, 0.8, 1.6 μM
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Incubation Time:48 h
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Result:Induced MNNG/HOS and MG63 cell apoptosis in a dose-dependent manner.
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Cell Line:MG63 and MNNG/HOS[1]
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Concentration:0, 0.1, 0.2, 0.4 μM
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Incubation Time:15 min
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Result:Inhibited the expression of α-tubulin in both MNNG/HOS and MG63 cells, inhibited proliferation and reduced the PDGFRβ fluorescence intensity in a concentration-dependent manner.
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Cell Line:MG63 and MNNG/HOS[1]
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Concentration:0, 0.1, 0.2, 0.4 μM
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Incubation Time:48 h
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Result:Effective inhibited PDGFRβ phosphorylation and downstream signaling transduction (p-STAT3, p-AKT, and p-ERK) at the cellular level.
PDGFR-IN-1 (C57/BL6 mice, 40, 80 mg/kg, orally, daily for 10 days) is safe for in vivo investigations[1].
PDGFR-IN-1 (Sprague-Dawley rats, 20 mg/kg PO or 4 mg/kg IP, once) shows a favorable profile with a high maximum concentration and exposure, an acceptable half-life , and a good oral bioavailability[1].
Pharmacokinetic Parameters of PDGFR-IN-1 in male Sprague-Dawley rats[1].
| 7m | ||
| route | IP | PO |
| dose (mg/kg) | 4 | 20 |
| Cmax (ng/mL) | 78.3 | 75.2 |
| t1/2 (h) | 2.86 | 2.12 |
| AUC0-∞ (ng/mL*h) | 211.3 | 664.7 |
| F (%) | 62.9 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley rats (male, 200-260 g, Six rats, two groups)[1]
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Dosage:20 mg/kg (PO) or 4 mg/kg (IP)
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Administration:PO, IP, once (Pharmacokinetic Analysis)
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Result:Showed a favorable profile with a high maximum concentration and exposure, an acceptable half-life , and a good oral bioavailability.
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Animal Model:BALB/c mice (18-20 g, MNNG/HOS xenograft mouse, eight groups)[1]
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Dosage:15, 30 mg/kg
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Administration:Orally, daily for 14 days
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Result:Significantly suppressed tumor growth, exhibited a stronger antitumor efficacy, did not cause significant body weight or organ weight (heart, lung, liver, spleen, or kidney) changes, strongly suppressed the proliferation of tumor cells and induced apoptosis in tissues of the tumor.
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Animal Model:C57/BL6 mice[1]
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Dosage:40, 80 mg/kg
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Administration:Orally, daily for 10 days
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Result:Did not reveal any obvious morphological aberration in organ tissues.
Chemical Information
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CAS No. 2644673-07-2
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Appearance Solid
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Molecular Weight 458.56
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Formula C25H30N8O
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Color Light yellow to brown
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SMILES
CC1=CN=C(N=C1NC2=CC3=C(C=C2)C=NN3)NC4=CC=C(C(OC)=C4)N5CCN(CC5)CC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (218.07 mM; Need ultrasonic; 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: ≥ 5 mg/mL (10.90 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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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 | 2.1807 mL | 10.9037 mL | 21.8074 mL | 54.5185 mL |
| 5 mM | 0.4361 mL | 2.1807 mL | 4.3615 mL | 10.9037 mL | |
| 10 mM | 0.2181 mL | 1.0904 mL | 2.1807 mL | 5.4518 mL | |
| 15 mM | 0.1454 mL | 0.7269 mL | 1.4538 mL | 3.6346 mL | |
| 20 mM | 0.1090 mL | 0.5452 mL | 1.0904 mL | 2.7259 mL | |
| 25 mM | 0.0872 mL | 0.4361 mL | 0.8723 mL | 2.1807 mL | |
| 30 mM | 0.0727 mL | 0.3635 mL | 0.7269 mL | 1.8173 mL | |
| 40 mM | 0.0545 mL | 0.2726 mL | 0.5452 mL | 1.3630 mL | |
| 50 mM | 0.0436 mL | 0.2181 mL | 0.4361 mL | 1.0904 mL | |
| 60 mM | 0.0363 mL | 0.1817 mL | 0.3635 mL | 0.9086 mL | |
| 80 mM | 0.0273 mL | 0.1363 mL | 0.2726 mL | 0.6815 mL | |
| 100 mM | 0.0218 mL | 0.1090 mL | 0.2181 mL | 0.5452 mL |
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