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GW2580

CAS No. : 870483-87-7

MCE 站：GW2580

产品活性：GW2580 是口服有效的，选择性的 c-Fms 激酶抑制剂，体外实验中在 0.06 μM 时可完全抑制人 cFMS 激酶。GW2580 是 ATP 与 cFMS 激酶结合的竞争性抑制剂，并且可以抑制集落刺激因子 1 信号传导。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：c-Fms

In Vitro: GW2580 completely inhibits the growth of CSF-1-dependent mouse myeloid M-NFS-60 cells at 0.7 μM. GW2580 at 0.8-1 μM completely blocks the ability of CSF-1 to induce the growth of mouse M-NFS60 myeloid cells and human monocytes.
GW2580 causes a 30-40% inhibition of PTH-induced calcium release at 0.1-0.3 μM, with higher concentrations of 1, 3, and 10 μM completely inhibiting the PTH response.
GW2580 inhibits CSF1R phosphorylation in RAW264.7 murine macrophages stimulated with 10 ng/mL with IC₅₀ of approximately 10 nM.
GW2580 also inhibits TRKA activity with IC₅₀ of 0.88 μM.

In Vivo: GW2580 (Oral administration; 20 and 80 mg/kg) produces a dose-related decrease in the number of tumor cells, with the 80 mg/kg dose completely blocking tumor growth.
GW2580 (Oral administration; 20 and 80 mg/kg) has gave maximal plasma concentrations of 1.4 and 5.6 μM, respectively.
GW2580 (50 mg/kg; twice a day from days 0 to 21, 7 to 21, or 14 to 21) inhibits joint connective tissue and bone destruction in a 21-day adjuvant arthritis model.

相关产品：Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Orally Active Compound Library  |  Ki20227  |  AZD7507  |  PLX647  |  cFMS Receptor Inhibitor II  |  CSF1R-IN-1

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