GW2580
目录号 : KM4945 CAS No. : 870483-87-7 纯度 : 98%

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。

规格 价格 是否有货 数量
10mg
In-stock
50mg
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100mg
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200mg
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500mg
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1g
In-stock
5g 询价 In-stock
10g 询价 In-stock

Other Forms of Rapamycin:

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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.

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.
分子式
C20H22N4O3
分子量
366.41
CAS号
870483-87-7
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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 17.5 mg/mL (47.76 mM; Need ultrasonic and warming)

Ethanol : < 1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7292 mL 13.6459 mL 27.2918 mL
5 mM 0.5458 mL 2.7292 mL 5.4584 mL
10 mM 0.2729 mL 1.3646 mL 2.7292 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.68 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.68 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.68 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.68 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.68 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.68 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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