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Ki11502

🥰Excellent
Catalog No. T208725Cas No. 347155-76-4

Ki11502 is a multi-target receptor tyrosine kinase (RTK) inhibitor that selectively inhibits the activity of PDGFβ/α receptors (with an IC50 of less than 10 nM). It specifically suppresses PDGFβ receptor phosphorylation, proliferation, and proteoglycan synthesis in human vascular smooth muscle cells. Additionally, Ki11502 induces apoptosis and exhibits significant antiproliferative effects against specific leukemia subgroups, including those with Imatinib-resistant mutations. It is particularly suitable for studying the role of PDGF in vascular diseases and the involvement of proteoglycans in atherosclerosis.

Ki11502

Ki11502

🥰Excellent
Catalog No. T208725Cas No. 347155-76-4
Ki11502 is a multi-target receptor tyrosine kinase (RTK) inhibitor that selectively inhibits the activity of PDGFβ/α receptors (with an IC50 of less than 10 nM). It specifically suppresses PDGFβ receptor phosphorylation, proliferation, and proteoglycan synthesis in human vascular smooth muscle cells. Additionally, Ki11502 induces apoptosis and exhibits significant antiproliferative effects against specific leukemia subgroups, including those with Imatinib-resistant mutations. It is particularly suitable for studying the role of PDGF in vascular diseases and the involvement of proteoglycans in atherosclerosis.
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Product Introduction

Bioactivity
Description
Ki11502 is a multi-target receptor tyrosine kinase (RTK) inhibitor that selectively inhibits the activity of PDGFβ/α receptors (with an IC50 of less than 10 nM). It specifically suppresses PDGFβ receptor phosphorylation, proliferation, and proteoglycan synthesis in human vascular smooth muscle cells. Additionally, Ki11502 induces apoptosis and exhibits significant antiproliferative effects against specific leukemia subgroups, including those with Imatinib-resistant mutations. It is particularly suitable for studying the role of PDGF in vascular diseases and the involvement of proteoglycans in atherosclerosis.
Targets&IC50
PDGFRβ:<10 nM, PDGFRα:<10 nM
In vitro
Ki11502, at concentrations of 0.1-1 nM and over a duration of 2 days, significantly induces growth arrest, G0/G1 cell cycle arrest, and apoptosis (Apoptosis) in eosinophilic leukemia EOL-1 cells carrying the activated FIP1-like 1/PDGFRα fusion gene. Additionally, Ki11502 reduces the levels of p-PDGFRα and its downstream signaling components, including p-Akt, p-ERK, and p-STAT5, in EOL-1 cells within 3 hours.
In vivo
Ki11502 administered at a dosage of 50 mg/kg, via oral gavage, twice daily for five consecutive days, completely inhibited the proliferation of EOL-1 tumor xenograft cells in SCID mice.
Chemical Properties
Molecular Weight473.54
FormulaC26H23N3O4S
Cas No.347155-76-4
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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