PX-478 2HCl
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
PX-478 2HCl也被称为PX-478，是一种实验用HIF-1α抑制剂。它抑制了常氧和缺氧肿瘤细胞株中HIF-1α蛋白的水平，IC50值大约为20-30 μM[1]。
缺氧诱导的转录因子HIF-1α激活参与糖酵解、红细胞生成和血管生成的靶基因。HIF-1α还调节编码细胞凋亡通路、生长因子/受体、细胞周期调节、转移和侵袭的基因[1]。
正常氧条件下，PC3细胞中PX-478抑制HIF-1α的IC50为20-25 μmol/L，而PX-478对DU145细胞中HIF-1α的抑制IC50大约为40-50 μmol/L。在DU 145和PC3细胞中，1小时低氧显著上调HIF-1α蛋白。但在1小时的缺氧诱导之前，使用PX-478常氧条件下预处理20小时，减弱了1小时缺氧诱导所累积的HIF-1α。在PC3细胞中，缺氧处理前，用20 μmol/L PX-478预处理，与单独缺氧处理相比，抑制了40％的HIF-1α。在DU 145细胞中，缺氧前用50 μmol/L PX-478预处理，与单独缺氧相比，抑制35％的HIF-1α[1]。
在C6报告基因异种移植nu/nu小鼠中，口服给药剂量为30 mg/kg的PX-478，持续2天，阻止了C6肿瘤的中央缺血区HIF-1的转录活性[2]。
参考文献：
[1]. Palayoor ST, Mitchell JB, Cerna D, et al. PX-478, an inhibitor of hypoxia-inducible factor-1α, enhances radiosensitivity of prostate carcinoma cells. International journal of cancer, 2008, 123(10): 2430-2437.
[2]. Schwartz DL, Powis G, Thitai-Kumar A, et al. The selective hypoxia inducible factor-1 inhibitor PX-478 provides in vivo radiosensitization through tumor stromal effects. Molecular cancer therapeutics, 2009, 8(4): 947-958.
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| Storage | Store at -20°C |
| M.Wt | 394.12 |
| Cas No. | 685898-44-6 |
| Formula | C13H20Cl4N2O3 |
| Solubility | ≥19.7 mg/mL in DMSO; ≥50 mg/mL in H2O; ≥8.42 mg/mL in EtOH |
| Chemical Name | (S)-4-(2-amino-2-carboxyethyl)-N,N-bis(2-chloroethyl)aniline oxide dihydrochloride |
| SDF | Download SDF |
| Canonical SMILES | ClCC[N+](C1=CC=C(C[C@@](N)([H])C(O)=O)C=C1)([O-])CCCl.Cl.Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验 [1]: | |
|
细胞系 |
DU145细胞 |
|
制备方法 |
在DMSO中的溶解度大于19.7 mg/mL。若配制更高浓度的溶液，一般步骤如下：请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。 |
|
反应条件 |
25 μM；18小时 |
|
实验结果 |
在缺氧条件下，给予PX-478，于18小时后可以增加DU145细胞的放射敏感性，但不会显著影响HIF-1α蛋白水平。 |
| 动物实验 [2]: | |
|
动物模型 |
携带C6报告基因异种移植瘤的裸鼠 |
|
给药剂量 |
30 mg/kg；口服给药；持续2天 |
|
实验结果 |
在携带C6报告基因异种移植瘤的裸鼠中，PX-478治疗（30 mg/kg；口服给药；持续2天）抑制C6肿瘤中心缺血区域HIF-1的转录活性。 |
|
注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同，但仍处于实验系统误差的允许范围内。 |
|
References: [1]. Palayoor ST, Mitchell JB, Cerna D, et al. PX-478, an inhibitor of hypoxia-inducible factor-1α, enhances radiosensitivity of prostate carcinoma cells. International journal of cancer, 2008, 123(10): 2430-2437. [2]. Schwartz DL, Powis G, Thitai-Kumar A, et al. The selective hypoxia inducible factor-1 inhibitor PX-478 provides in vivo radiosensitization through tumor stromal effects. Molecular cancer therapeutics, 2009, 8(4): 947-958. |
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质量控制和MSDS
- 批次:
化学结构
相关生物数据
相关生物数据
