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PDGFR-IN-1

Name: PDGFR-IN-1
Brand: TargetMol
SKU: T62872
Price: 189 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T62872Cas No. 2644673-07-2

PDGFR-IN-1 is an orally active, highly efficient platelet-derived growth factor receptor (PDGFR) inhibitor with potent antitumor activity. It inhibits PDGFRα and PDGFRβ and can be used in solid tumor research.

PDGFR-IN-1

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Purity: 99.49%

Catalog No. T62872Cas No. 2644673-07-2

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$189	-	In Stock
5 mg	$479	-	In Stock
10 mg	$728	-	In Stock
25 mg	$1,280	-	In Stock
50 mg	$1,850	-	In Stock
100 mg	$2,500	-	In Stock
1 mL x 10 mM (in DMSO)	$483	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.49%

Appearance:Solid

Color:White

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COA HNMR HPLC

Product Introduction

Bioactivity

Description	PDGFR-IN-1 is an orally active, highly efficient platelet-derived growth factor receptor (PDGFR) inhibitor with potent antitumor activity. It inhibits PDGFRα and PDGFRβ and can be used in solid tumor research.
Targets&IC50	PDGFRα:2.4 nM, PDGFRβ:0.9 nM
In vitro	PDGFR-IN-1 is a potent inhibitor of PDGFR (platelet-derived growth factor receptor) with IC50 of 2.4 and 0.9 nM for PDGFRα and PDGFRβ, respectively. PDGFR-IN-1 showed the highest antiproliferative activity against human osteosarcoma cancer cell lines with abnormal PDGFRα and/or PDGFRβ activation (MG63, U2OS, MNNG/HOS, and SAOS-2). The IC50 values were 0.44, 0.42, 1.03 and 0.37 μM, respectively. PDGFR-IN-1 (0.1, 0.2, and 0.4 μM) inhibited α-tubulin expression IN MNNG/HOS and MG63 cells in a dose-dependent manner, thereby inhibiting cancer cell formation. PDGFR-IN-1 inhibits PDGFRβ phosphorylation and downstream signal transduction (p-STAT3, p-AKT, and p-ERK) IN MNNG/HOS cells. PDGFR-IN-1 significantly inhibits the migration and invasion of osteosarcoma cancer cells by down-regulating the expression of FAK and its distribution on the cell front. [1]
In vivo	Orally administered PDGFR-IN-1 (40, 80 mg/kg/ day for 10 days), the mice showed good resistance. IN a MNNG/HOS xenograft mouse model, PDGFR-IN-1 (30 mg/kg for 14 days) treatment significantly inhibited tumor growth. [1]

Chemical Properties

Molecular Weight	458.56
Formula	C₂₅H₃₀N₈O
Cas No.	2644673-07-2
Smiles	N1=CC=2C=CC(=CC2N1)NC3=NC(=NC=C3C)NC4=CC=C(C(OC)=C4)N5CCN(CC)CC5

Storage & Solubility Information

Storage

keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 80 mg/mL (174.46 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (10.9 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1807 mL	10.9037 mL	21.8074 mL	109.0370 mL
5 mM	0.4361 mL	2.1807 mL	4.3615 mL	21.8074 mL
10 mM	0.2181 mL	1.0904 mL	2.1807 mL	10.9037 mL
20 mM	0.1090 mL	0.5452 mL	1.0904 mL	5.4518 mL
50 mM	0.0436 mL	0.2181 mL	0.4361 mL	2.1807 mL
100 mM	0.0218 mL	0.1090 mL	0.2181 mL	1.0904 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

PDGFR-IN-1

PDGFR-IN-1

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In Vivo Formulation Calculator (Clear solution)

Dose Conversion

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