Ki20227

Catalog No.S7688 Batch:S768801

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Technical Data

Formula

C24H24N4O5S

Molecular Weight 480.54 CAS No. 623142-96-1
Solubility (25°C)* In vitro DMSO 96 mg/mL (199.77 mM)
Ethanol 3 mg/mL (6.24 mM)
Water ˂1 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Ki20227 is an orally active and highly selective inhibitor of c-Fms tyrosine kinase(CSF1R) with IC50 of 2 nM, 12 nM, 451 nM and 217 nM for c-Fms, vascular endothelial growth factor receptor-2 (KDR/VEGFR-2), stem cell factor receptor (c-Kit), and platelet-derived growth factor receptor beta (PDGFRβ), respectively.
Targets
c-Fms [1]
(Cell-free assay)
VEGFR2 [1]
(Cell-free assay)
PDGFRβ [1]
(Cell-free assay)
c-Kit [1]
(Cell-free assay)
2 nM 12 nM 217 nM 451 nM
In vitro

Ki20227, a novel quinoline-urea derivative, is a c-Fms tyrosine kinase inhibitor. The IC50s of Ki20227 to inhibit c-Fms, vascular endothelial growth factor receptor-2 (KDR), stem cell factor receptor (c-Kit), and platelet-derived growth factor receptor B are found to be 2, 12, 451, and 217 nmol/L, respectively. Ki20227 is also found to inhibit the M-CSFdependent growth of M-NFS-60 cells but not the M-CSFindependent growth of A375 human melanoma cells in vitro. Furthermore, in an osteoclast-like cell formation assay using mouse bone marrow cells, Ki20227 inhibits the development of tartrate-resistant acid phosphatase-positive osteoclast-like cells in a dose-dependent manner.[1]

In vivo

In in vivo studies, oral administration of Ki20227 suppresses osteoclast-like cell accumulation and bone resorption induced by metastatic tumor cells in nude rats following intracardiac injection of A375 cells. Moreover, Ki20227 decreases the number of tartrate-resistant acid phosphatase–positive osteoclast-like cells on bone surfaces in ovariectomized (ovx) rats. These findings suggest that Ki20227 inhibits osteolytic bone destruction through the suppression of M-CSF-induced osteoclast accumulation in vivo.[1]

Protocol (from reference)

Cell Assay:

[1]

  • Cell lines

    RAW264.7, M-NFS-60, A375, HUVEC cells

  • Concentrations

    0.1 nM - 3000 nM

  • Incubation Time

    72 h, 1h

  • Method

    M-NFS-60, HUVEC, and A375 cells are seeded on a 96-well culture plate and cultured for 24 hours. Then, culture mediums are changed and incubated for a further 72 hours in the presence or absence of Ki20227 (0.1–3,000 nmol/L).
    RAW264.7 cells are serum starved for 12 hours in DMEM containing 0.1% FCS. Serial dilutions of Ki20227 are then added to the cells, and they are incubated for 1 hour. RAW264.7 cells are stimulated with 50 ng/mL of recombinant mouse M-CSF for 4 minutes. c-Fms protein in the RAW264.7 cell lysate is prepared with ice-cold lysis buffer.

Animal Study:

[1]

  • Animal Models

    Athymic rats (F344/NJcl-rnu), Sprague-Dawley rats

  • Dosages

    20 mg/kg

  • Administration

    Oral gavage

Selleck's Ki20227 has been cited by 2 publications

PGRN inhibits CD8+T cell recruitment and promotes breast cancer progression by up-regulating ICAM-1 on TAM [ Cancer Immunol Immunother, 2024, 73(5):76] PubMed: 38554213
PGRN inhibits CD8+T cell recruitment and promotes breast cancer progression by up-regulating ICAM-1 on TAM [ Cancer Immunol Immunother, 2024, 73(5):76] PubMed: 38554213

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.