PX-478 2HCl |
| カタログ番号GC11031 |
PX-478は、構成的および低酸素誘導性のHIF-1αレベルを抑制する選択的阻害剤である。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 685898-44-6
Sample solution is provided at 25 µL, 10mM.
PX-478は、構成的および低酸素誘導性のHIF-1αレベルを抑制する選択的阻害剤である。PX-478は、HIF-1αの翻訳の阻害およびHIF-1α mRNAレベルの低下を含む複数のレベルでHIF-1αを抑制する。PX-478は、いくつかの攻撃的なヒト腫瘍異種移植片に対して抗腫瘍活性も示している。
in vitroおよびin vivo研究は、PX-478が常酸素および低酸素誘導性のHIF-1α発現、炎症分子COX-2および免疫抑制分子PD-L1の発現を抑制できることを示した。したがって、PX-478は、腫瘍の発生に対する広範な効果を示し、増殖の抑制、細胞アポトーシスの促進、EMTプロセスの抑制、および細胞周期の停止などがある。in vivo実験では、PX-478の腫瘍成長に対する抑制効果が示された。
References:
[1].Zhu Y, et al. Inhibition of HIF-1α by PX-478 suppresses tumor growth of esophageal squamous cell cancer in vitro and in vivo. Am J Cancer Res. 2017 May 1;7(5):1198-1212.
[2].Palayoor ST, et al. PX-478, an inhibitor of hypoxia-inducible factor-1alpha, enhances radiosensitivity of prostate carcinoma cells. Int J Cancer. 2008 Nov 15;123(10):2430-7.
| 細胞実験[1]: | |
細胞株 | EC109 および EC9706 細胞株 |
準備方法 | 両細胞株は、5% CO2 加湿インキュベーター内で 37°C で 10% FBS を添加した RPMI 1640 で培養された。細胞は、処理前に 0.1% FBS を含む培地で 24 時間飢餓状態にされた。 |
反応条件 | 一晩血清飢餓状態にした後、PX-478 を最終濃度 20 umol/L になるように培養物に加えた。 |
アプリケーション | PX-478 は、EC9706 および EC109 細胞で 20 μM の用量で、in vitro で常酸素および低酸素誘導性 HIF-1α 発現、ならびに COX-2 および PD-L1 発現を阻害できる。標的 HIF-1α は、それらの発現を効果的に低減できる。 |
| 動物実験 [1]: | |
動物モデル | 6 週齢のメス BALB/c ヌードマウス、18 ± 2 g、SPF グレード |
準備方法 | EC109 細胞を PBS に 107/mL で再懸濁した。合計 12 匹のメス BABL/c ヌードマウスを使用した。マウスの右脇腹に EC109 細胞を注入して腫瘍異種移植を確立した。各グループの 12 匹の腫瘍を持つマウスを、コントロール グループと PX-478 グループにランダムに分けた。すべての薬剤は経口投与で投与した。 |
投与形態 | 1 日おきに 30 mg/kg |
アプリケーション | PX-478 は、増殖の抑制、細胞のアポトーシスの促進、EMT プロセスの阻害、細胞周期の停止など、腫瘍の発達に幅広い効果を示す。in vivo マウス異種移植モデルでは、腫瘍の成長に対する阻害効果が示された。さらに、COX-2およびPD-L1の発現を低下させることもできる。 |
参考文献: [1].Zhu Y, et al. Inhibition of HIF-1α by PX-478 suppresses tumor growth of esophageal squamous cell cancer in vitro and in vivo. Am J Cancer Res. 2017 May 1;7(5):1198-1212. | |
| Cas No. | 685898-44-6 | SDF | |
| Chemical Name | (S)-4-(2-amino-2-carboxyethyl)-N,N-bis(2-chloroethyl)aniline oxide dihydrochloride | ||
| Canonical SMILES | ClCC[N+](C1=CC=C(C[C@@](N)([H])C(O)=O)C=C1)([O-])CCCl.Cl.Cl | ||
| Formula | C13H20Cl4N2O3 | M.Wt | 394.12 |
| 溶解度 | 79mg/mL in DMSO (200.45mM), 79mg/mL in Water (200.45mM), 79mg/mL in Ethanol (200.45mM) | Storage | Store at -20°C, stored under nitrogen, away from moisture |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5373 mL | 12.6865 mL | 25.373 mL |
| 5 mM | 0.5075 mL | 2.5373 mL | 5.0746 mL |
| 10 mM | 0.2537 mL | 1.2686 mL | 2.5373 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)
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