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抑制剂/激活剂

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凋亡与自噬

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GW2580

GW2580 (SC-203877) 是一种选择性CSF-1R抑制剂，作用于c-FMS时，IC50为30 nM，比作用于b-Raf， CDK4， c-KIT， c-SRC， EGFR， ERBB2/4， ERK2， FLT-3， GSK3， ITK， JAK2等的选择性高150到500倍。

货号：
TK0438
规格：

1mg

|10mg

50mg
价格：
￥0.00

产品参数

CAS No.	870483-87-7
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.
分子式	C20H22N4O3
分子量	366.41
储存条件	Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶解性数据	DMSO : 33.33 mg/mL (90.96 mM; Need ultrasonic) Ethanol : < 1 mg/mL (insoluble)
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.
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.

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