GW2580|870483-87-7|-陌孚医药/Medlife

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GW2580

目录号: PL01774 纯度: ≥99%

CAS No. :870483-87-7

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中文名称	GW2580
中文别名	5-[3-甲氧基-4-(4-甲氧基苄氧基)苄基]嘧啶-2,4-二胺;Fmoc-3-1-羧甲基-2-戊内酰胺;GW2580 抑制剂;5-[3-甲氧基-4-[(4-甲氧基苄基)氧]苄基]嘧啶-2,4-二胺
英文名称	GW2580
英文别名	5-[3-Methoxy-4-(4-methoxybenzyloxy)benzyl]pyrimidine-2,4-diamine;5-[3-Methoxy-4-(4-methoxy-benzyloxy)-benzyl]-pyrimidine-2,4-diamine;GW2580;5-[[3-methoxy-4-[(4-methoxyphenyl)methoxy]phenyl]methyl]pyrimidine-2,4-diamine;cFMS Receptor Tyrosine Kinase Inhibitor;GW-2580;GW2580, FREE BASE;PLX-0728;2,4-Pyrimidinediamine,5-((3-methoxy-4-((4-methoxyphenyl)methoxy)phenyl)methyl);4at5;5-(3-Methoxy-4-((4-methoxybenzyl)oxy)benzyl)-pyrimidine-2,4-diamine;CSF-1 Receptor Inhibitor;Kinome_3757;5-[[3-Methoxy-4-[(4-methoxyphenyl)methoxy]phenyl]methyl]-2,4-Pyrimidinediamine;5-[3-Methoxy-4-[(4-methoxybenzyl)oxy]benzyl]pyrimidine-2,4-diamine;GW 2580;GW632580X;SRV0JCF9LI;5-{3-methoxy-4-[(4-methoxybenzyl)oxy]benzyl}pyrimidine-2,4-diamine;5-(3-Methoxy-4-((4-methoxybenzyl)oxy)benzyl)pyrimidine-2,4-diamine;5-(3-METHOXY-4-(4-METHOXYBENZYLOXY)BENZYL)PYRIMIDINE-2,4-DIAMINE;2,4-Pyrimidinediamine, 5-((3-methoxy-4-((4-methoxyphenyl)methoxy)phenyl)methyl)-;CSF-1 Rece;5-[[3-Methoxy-4-[(4-methoxyphenyl)methoxy]phenyl]methyl]pyrimidine-2,4-diamine
Cas No.	870483-87-7
分子式	C₂₀H₂₂N₄O₃
分子量	366.41
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	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。
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.
性状	Solid
IC50 & Target[1][2]	IC50: 60 nM (c-FMS)
体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Conway JG, et al. Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580. Proc Natl Acad Sci U S A. 2005 Nov 1;102(44):16078-83. [2]. Priceman SJ, et al. Targeting distinct tumor-infiltrating myeloid cells by inhibiting CSF-1 receptor: combating tumor evasion of antiangiogenic therapy. Blood. 2010 Feb 18;115(7):1461-71

溶解度数据	In Vitro: DMSO : 33.33 mg/mL (90.96 mM; Need ultrasonic)Ethanol : < 1 mg/mL (insoluble)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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