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PDGFR-IN-1
🥰Excellent
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
🥰Excellent
Purity: 99.49%
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.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $189 | In Stock | |
| 5 mg | $479 | In Stock | |
| 10 mg | $766 | In Stock | |
| 25 mg | $1,520 | In Stock | |
| 50 mg | $1,980 | In Stock | |
| 100 mg | $2,500 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $483 | In Stock |
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Purity:99.49%
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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.Product Introduction
Bioactivity
Chemical Properties
| 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] |
| 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. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 80 mg/mL (174.46 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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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 mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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