PX-478 2HCl |
| Catalog No.GC11031 |
PX-478은 상성적 및 낮은 산소 환경에서 hypoxia-induced HIF-1 α수준을 억제하는 선택적 억제제이다.
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.
Product has been cited by 4 publications
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Related Biological Data
Effects of ononin combined with radiation on tumor growth and tumor cell apoptosis in human lung cancer subcutaneous tumor-bearing nude mice model. (D) Representative images of Hematoxylin-eosin (H&E) staining, Ki67 immunohistochemical staining (Scar bars = 40 µm) and TUNEL staining.
PX-478 was purchased from GLPBIO (GC11031, GLPBIO,Montclair, USA),(40mg/kg, 0.2ml, ip).
Phytomedicine 125 (2024): 155290. PMID: 38308918 IF: 7.8996 -
Related Biological Data
(c) Quantitative comparison of the number of CD31+ vessels between TCPS with PX-478 or PBS injection after implantation in FVB mice at 14 d per FOV.
The post-surgery mice were administered of PX478 (100mg kg -1)(GlpBio, USA) in phosphate buffer solution (PBS) every other day for a total of 2 weeks according to Agarwal’s protocol.
J Mater Chem B (2022). PMID: 35971918 IF: 7.5711 -
Related Biological Data
Inhibition of HIF-1α signaling alleviated FA-induced glycolysis in PMs. B, intracellular MGO levels was demonstrated by the mean fluorescence intensity of NAP-DCP-1.
RAW 264.7 cells were pretreated with 30μM PX-478(GlpBio, USA)(a specific HIF-1α inhibitor) for 24h to block HIF-1α signaling.
Chem-Biol Interact 379 (2023): 110514. PMID: 37105513 IF: 5.1 -
Related Biological Data
CM from FA-treated tumor cells and MGO promoted TAM polarization. B, % of M2 TAM measured by CD163+ CD206+ double positive population.
Hela cells were treated with 0, 20, 50μM FA or 50μM FA + 5μM PX-478 (HIF-1α inhibitor)(GlpBio, USA) for 24h.
Toxicol Appl Pharm (2022): 115910. PMID: 35134435 IF: 4.219
Product Documents
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Protocol
| 세포 실험 [1]: | |
세포 라인 | EC109 및 EC9706 세포 라인 |
제조 방법 | 두 세포 라인 모두 37°C, 5% CO2의 습도 조절 인큐베이터에서 10% 태우선혈청을 추가한 RPMI 1640 배양액으로 배양되었습니다. 처리 전에 세포는 0.1% FBS를 포함하는 매체에서 24시간 동안 배고 상태를 유지했습니다. |
반응 조건 | 혈청 배고 상태를 유지한 다음 PX-478은 최종 농도 20 umol/L로 배양물에 추가되었습니다. |
응용 분야 | PX-478은 EC9706 및 EC109 세포에서 정상 산소 조건과 희석 조건에서 HIF-1α 표현을 억제할 수 있으며, COX-2 및 PD-L1 표현도 억제할 수 있습니다. 이 실험의 용액 농도는 20 μM입니다. 표적 HIF-1α는 그들의 표현을 효과적으로 감소시킬 수 있습니다. |
| 동물 실험 [2]: | |
동물 모형 | 6주령의 암컷 BALB/c 누드 쥐, 체중 18 ± 2g, SPF 등급 |
제조 방법 | EC109 세포는 PBS에서 107/mL의 농도로 재정지되었습니다. 총 12마리의 BALB/c 무모 쥐 암컷이 사용되었습니다. 쥐는 우측 복부 영역에 EC109 세포를 주사하여 종양 이종 이식 모델을 구축하였습니다. 각 그룹의 12마리의 종양 이식 쥐는 무작위로 대조군과 PX-478 그룹으로 나뉘었습니다. 모든 약물은 구강 투여로 전달되었습니다. |
제형 | 매 번 30mg/kg |
응용 분야 | PX-478은 종양 발전에 광범위한 영향을 미칩니다. 예를 들어, 증식을 억제하고 세포 조각사를 촉진하며, EMT 과정을 억제하고, 세포 주기를 중단합니다. 체내 쥐 이종 이식 모델에서는 종양 성장에 대한 억제 효과를 나타냈습니다. 또한, COX-2 및 PD-L1 표현을 감소시킬 수 있습니다. |
참고문헌: [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. | |
PX-478은 상성적 및 낮은 산소 환경에서 hypoxia-induced HIF-1 α수준을 억제하는 선택적 억제제이다.PX-478은 HIF-1α의 번역을 억제하고 HIF-1α mRNA 수준을 낮추는 것을 포함하여 여러 수준에서 HIF-1α를 억제한다. [1] PX-478은 또한 몇 가지 공격적인 인간의 종양 xenografts에 대한 항종양 활동을 보여주었다. [2]
체외및 체내 연구는 PX-478이 정상 산소 상태와 낮은 산소 유도 HIF-1α 표현, inflammatory molecule COX-2 및 면역억제 분자 PD-L1 표현을 모두 억제할 수 있음을 보여줌. 따라서 PX-478은 증식을 억제하고, 세포 조기 죽음을 촉진하며, EMT 과정을 억제하고, 세포 주기를 중단하는 등 종양 발전에 넓은 영향을 미칠 수 있음을 보여준다. 체내 실험은 PX-478이 종양 성장에 대한 억제 효과를 나타냈다. [1]
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.
| 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 |
| Solubility | 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. | ||
Complete Stock Solution Preparation Table
| 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 |
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Related Video
PX-478 2HCl-GlpBio
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