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。
| 生物活性 | Tyrphostin AG1296 is a potent and selective inhibitor ofplatelet-derived growth factor receptor (PDGFR), with anIC50of 0.8 μM. Tyrphostin AG1296 inhibits signaling of humanPDGFα-andβ-receptorsas well as of the relatedstem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor ofFLT3, with anIC50in the micromolar range[1][2][3]. |
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体外研究
(In Vitro) | Tyrphostin AG1296 (0.625-20 μM; 72 h) suppresses viability of PLX4032-resistant melanoma cells[4].
Tyrphostin AG1296 (2.5-20 μM; 48 h) induces apoptosis of A375R cells[4].
Tyrphostin AG1296 (5 and 20 μM; 2 h) inhibits PDGFR phosphorylation in A375R cells[4].
Tyrphostin AG1296 (0.0625-1 μM; 8 h) inhibits migration of A375R cells[4].
Cell Viability Assay[4] | 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[4] | 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[4] | Cell Line: | A375R cells | | Concentration: | 5, 20 μM | | Incubation Time: | 2 h | | Result: | Inhibited phosphorylation of both PDGFR-α and PDGFR-β. |
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体内研究
(In Vivo) | Tyrphostin AG1296 (40 and 80 mg/kg; i.p. daily for two weeks) suppresses A375R tumor growth in vivo[4].
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[5].
| Animal Model: | Nud/nud mice are injected with A375R cells[4] | | 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. |
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : 33.33 mg/mL(125.16 mM;Need ultrasonic) 配制储备液 | 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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-CDin 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 μL20% 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。
*以上所有助溶剂都可在本网站选购。 |
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