产品说明书
PT2399
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同义名 : | - |
| CAS号 : | 1672662-14-4 | |
| 货号 : | A1176640 | |
| 分子式 : | C17H10F5NO4S | |
| 纯度 : | 98% | |
| 分子量 : | 419.323 | |
| MDL号 : | MFCD32062659 | |
| 存储条件： |
粉末 Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 190 mg/mL(453.11 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | PT2399 is a potent and selective HIF-2α antagonist that directly binds to the HIF-2α PAS B domain with an IC50 value of 6 nM. PT2399 has shown potent antitumour activity in vivo[1][2][3].PT2399 directly binds to the HIF-2α PAS B domain and impairs the ability of HIF-2α to bind to the aromatic hydrocarbon receptor nuclear transporter (ARNT)[2].At a concentration of 20 μM, PT2399 inhibited the proliferation of HIF-2α -/- 786-O cells and other cancer cell lines in which HIF-2α was undetectable, suggesting that PT2399 leads to off-target toxicity. PT2399 inhibited a variety of HIF-targeted genes in 786-O VHL-/- ccRCC cells, but not HIF-1α-specific target genes such as BNIP3[2]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.38mL 0.48mL 0.24mL |
11.92mL 2.38mL 1.19mL |
23.85mL 4.77mL 2.38mL |
| 参考文献 |
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