2. Protein Tyrosine Kinase/RTK Apoptosis
  3. PDGFR Apoptosis
  4. PDGFR-IN-1

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.

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PDGFR-IN-1 Chemical Structure

PDGFR-IN-1 Chemical Structure

CAS No. : 2644673-07-2

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

PDGFR-IN-1 Related Antibodies

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Description

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[1].

IC50 & Target

IC50: 2.4 nM (PDGFRα), 0.9 nM (PDGFRβ)[1]
Cellular Effect
Cell Line Type Value Description References
HOS-TE85 IC50
1.03 μM
Compound: 7m
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
[PMID: 35239349]
MG-63 IC50
0.44 μM
Compound: 7m
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
[PMID: 35239349]
SAOS-2 IC50
0.37 μM
Compound: 7m
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
[PMID: 35239349]
U2OS IC50
0.42 μM
Compound: 7m
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
[PMID: 35239349]
In Vitro

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.

PDGFR-IN-1 Related Antibodies

Cell Proliferation Assay

Cell Line: Human osteosarcoma cancer cell lines (U2OS, MG63, MNNG/HOS, and SAOS-2)[1]
Concentration: 0.1, 0.2, and 0.4 μM.
Incubation Time: 48 h
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.

Cell Cycle Analysis

Cell Line: MG63 and MNNG/HOS cells[1]
Concentration: 0, 0.1, 0.2, 0.4 μM
Incubation Time: 48 h
Result: Induced G2/M cell-cycle arrest in MNNG/HOS and G0/G1 cell-cycle arrest in MG63 cells in a dose-dependent manner.

Apoptosis Analysis

Cell Line: MG63 and MNNG/HOS cells[1]
Concentration: 0, 0.4, 0.8, 1.6 μM
Incubation Time: 48 h
Result: Induced MNNG/HOS and MG63 cell apoptosis in a dose-dependent manner.

Immunofluorescence

Cell Line: MG63 and MNNG/HOS[1]
Concentration: 0, 0.1, 0.2, 0.4 μM
Incubation Time: 15 min
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.

Western Blot Analysis

Cell Line: MG63 and MNNG/HOS[1]
Concentration: 0, 0.1, 0.2, 0.4 μM
Incubation Time: 48 h
Result: Effective inhibited PDGFRβ phosphorylation and downstream signaling transduction (p-STAT3, p-AKT, and p-ERK) at the cellular level.
In Vivo

PDGFR-IN-1 (BALB/c mice, MNNG/HOS xenograft mouse, 15, 30 mg/kg, orally, daily for 14 days) significantly suppresses tumor growth, exhibits a stronger antitumor efficacy with low toxicity[1].
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.

Animal Model: Sprague-Dawley rats (male, 200-260 g, Six rats, two groups)[1]
Dosage: 20 mg/kg (PO) or 4 mg/kg (IP)
Administration: PO, IP, once (Pharmacokinetic Analysis)
Result: Showed a favorable profile with a high maximum concentration and exposure, an acceptable half-life , and a good oral bioavailability.
Animal Model: BALB/c mice (18-20 g, MNNG/HOS xenograft mouse, eight groups)[1]
Dosage: 15, 30 mg/kg
Administration: Orally, daily for 14 days
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.
Animal Model: C57/BL6 mice[1]
Dosage: 40, 80 mg/kg
Administration: Orally, daily for 10 days
Result: Did not reveal any obvious morphological aberration in organ tissues.
Molecular Weight

458.56

Formula

C25H30N8O
CAS No.
Appearance

Solid

Color

Light yellow to brown

SMILES

CC1=CN=C(N=C1NC2=CC3=C(C=C2)C=NN3)NC4=CC=C(C(OC)=C4)N5CCN(CC5)CC
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 : 100 mg/mL (218.07 mM; Need ultrasonic; 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 2.1807 mL 10.9037 mL 21.8074 mL
5 mM 0.4361 mL 2.1807 mL 4.3615 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

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

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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: ≥ 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.
In Vivo Dissolution Calculator
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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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, 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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PDGFR-IN-1 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:

PDGFR-IN-12644673-07-2PDGFRApoptosisPlatelet-derived growth factor receptorOsteosarcomaMG63 cellMNNG/HOS cellLow toxicityBioavailabilityMetabolic stabilityOrally activeInhibitorinhibitorinhibit

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