产品
编 号：F489421
分子式：C20H22N4O3
分子量：366.41
分子式：C20H22N4O3
分子量：366.41
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
188
In-stock
5mg
375
In-stock
10mg
600
In-stock
50mg
1760
In-stock
100mg
2800
In-stock
200mg
4331
In-stock
结构图
CAS No: 870483-87-7
产品详情
生物活性：
GW2580 is an orally bioavailable and selective inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 acts as a competitive inhibitor of ATP binding to the cFMS kinase and inhibits colony-stimulating-factor-1 signaling.
体内研究：
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.Animal Model:Female C3H/HEN mice or female CD-1 nude mice weighing 22-26 g
Dosage:20 and 80 mg/kg
Administration:Oral administration
Result:Produced a dose-related decrease in the number of tumor cells, with the 80 mg/kg dose completely blocking tumor growth.
Animal Model:Female C3H/HEN mice or female CD-1 nude mice weighing 22-26 g
Dosage:20 and 80 mg/kg (Pharmacokinetic Study)
Administration:Oral administration
Result:Had gave maximal plasma concentrations of 1.4 and 5.6 μM, respectively.
体外研究：
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.
GW2580 is an orally bioavailable and selective inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 acts as a competitive inhibitor of ATP binding to the cFMS kinase and inhibits colony-stimulating-factor-1 signaling.
体内研究：
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.Animal Model:Female C3H/HEN mice or female CD-1 nude mice weighing 22-26 g
Dosage:20 and 80 mg/kg
Administration:Oral administration
Result:Produced a dose-related decrease in the number of tumor cells, with the 80 mg/kg dose completely blocking tumor growth.
Animal Model:Female C3H/HEN mice or female CD-1 nude mice weighing 22-26 g
Dosage:20 and 80 mg/kg (Pharmacokinetic Study)
Administration:Oral administration
Result:Had gave maximal plasma concentrations of 1.4 and 5.6 μM, respectively.
体外研究：
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.
产品资料
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