Tyrphostin AG1296 (Synonyms:AG1296)
目录号 : KM6762 CAS No. : 146535-11-7 纯度 : 98%

Tyrphostin AG1296 是一种有效的、选择性血小板衍生生长因子受体 (PDGFR) 抑制剂,IC50 值为 0.8 μM。Tyrphostin AG1296 抑制人 PDGF α 和 β 受体以及相关干细胞因子受体 (c-Kit) 的信号传导。Tyrphostin AG1296 也是有效的 FLT3 抑制剂,IC50 值在微摩尔范围内。

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5mg
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10mg
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25mg
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50mg
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100mg
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200mg 询价 In-stock
500mg 询价 In-stock

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生物活性

Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range.

体外研究

Tyrphostin AG1296 (0.625-20 μM; 72 h) suppresses viability of PLX4032-resistant melanoma cells.
Tyrphostin AG1296 (2.5-20 μM; 48 h) induces apoptosis of A375R cells.
Tyrphostin AG1296 (5 and 20 μM; 2 h) inhibits PDGFR phosphorylation in A375R cells.
Tyrphostin AG1296 (0.0625-1 μM; 8 h) inhibits migration of A375R cells.

Cell Viability Assay

Cell Line: PLX4032-resistant cell lines (A375R and SK-MEL-5R)
Concentration: 0.625, 1.25, 5, 20 μM
Incubation Time: 72 h
Result: Reduced the viability of both PLX4032-sensitive and PLX4032-resistant cell lines.

Apoptosis Analysis

Cell Line: A375R cells
Concentration: 2.5, 5, 10, 20 μM
Incubation Time: 48 h
Result: Induced dramatic apoptosis in A375R cells.

Western Blot Analysis

Cell Line: A375R cells
Concentration: 5, 20 μM
Incubation Time: 2 h
Result: Inhibited phosphorylation of both PDGFR-α and PDGFR-β.
体内研究

Tyrphostin AG1296 (40 and 80 mg/kg; i.p. daily for two weeks) suppresses A375R tumor growth in vivo.
Tyrphostin AG1296 (2 mg/kg; i.p. every other day for 3 weeks) inhibits the atherosclerotic plaque progression and enhances plaque stability by inhibiting inflammatory responses, reducing the expression of matrix metalloproteinases and promoting macrophages from proinflammatory phenotype to anti-inflammatory phenotype.

Animal Model: Nud/nud mice are injected with A375R cells
Dosage: 40, 80 mg/kg
Administration: I.p. daily for two weeks
Result: Led to an intermediate level of tumor growth suppression at dose of 40 mg/kg, and significant inhibition of A375R tumor growth at dose of 80 mg/kg.
Well tolerated by healthy mice without significant signs of overt toxicity or weight loss.
分子式
C16H14N2O2
分子量
266.29
CAS号
146535-11-7
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 : 33.33 mg/mL (125.16 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.7553 mL 18.7765 mL 37.5530 mL
5 mM 0.7511 mL 3.7553 mL 7.5106 mL
10 mM 0.3755 mL 1.8777 mL 3.7553 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    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (9.39 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (9.39 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 25.0 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。

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (9.39 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.39 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

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