PX-478 NEW
| Price | $48 | $81 | $139 |
| Package | 2mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-15 |
Product Details
| Product Name: PX-478 | CAS No.: 685898-44-6 |
| Purity: ≥98% | Supply Ability: 10g |
| Release date: 2024/11/15 |
Product Introduction
Bioactivity
| 名稱 | PX-478 |
| 描述 | PX-478 is a HIF-1α inhibitor with selectivity, oral activity, and blood-brain barrier permeability. PX-478 has antitumor activity and also protects pancreatic β-cell function in diabetes mellitus and is used in type 2 diabetes mellitus research. |
| 細胞實驗 | PX-478 is prepared as a 10 mM stock in distilled water and used immediately[1]. To determine the effect of PX-478 in combination with radiation, cells are treated with PX-478 for 24 hr under normoxic condition, irradiated and plated after 1 hr. Colonies are stained with crystal violet after 12 days and the colonies of >50 cells are counted. For combination treatments, net survival is calculated by correcting the toxicity of PX-478 alone. Enhancement factor (EF) is calculated by dividing the dose of radiation required to reduce plating efficiency to 10% when cells are treated with radiation alone by the dose of radiation required to reduce plating efficiency to 10% when cells are treated with PX-478 and radiation[1]. |
| 體外活性 | METHODS: Tumor cells MCF-7, HT-29 and PC-3 were treated with PX-478 under normoxic or hypoxic conditions for 16 h, and then grown under normoxic conditions for another 56 h. Cell viability was detected by MTT assay. RESULTS: PX-478 produced a smaller but significantly greater inhibition of cell growth under hypoxic conditions compared to normoxic conditions. the hypoxic/normoxic IC50 of MCF-7 cells was 25.1/20.0 μM, with a ratio of 1.25. the hypoxic/normoxic IC50 of HT-29 cells was 29.5/23.9 μM, with a ratio of 1.20, and that of PC-3 cells was 16.2/11.9 μM, with a ratio of 16.2/11.0 μM. IC50 for PC-3 cells was 16.2/11.1 μM with a ratio of 1.45. [1] METHODS: Human prostate cancer cells PC3 and DU 145 were treated with PX-478 (10-40 μM) under normoxic conditions for 20 h. The expression levels of target proteins were detected by Western Blot. RESULTS: Under normoxic conditions, the IC50 of PX-478 for HIF-1α inhibition in PC3 cells was 20-25 μM (ΔHIF:0.56±0.08), while the IC50 of HIF1α inhibition in DU 145 cells was 40-50 μM (ΔHIF:0.47±0.08). [2] |
| 體內(nèi)活性 | METHODS: To study the activity on metabolism in vivo, PX-478 (5 mg/kg) was administered by gavage to C57BL/6 mice on a high-fat diet (HFD) every two days for seven weeks. RESULTS: PX-478 treatment effectively inhibited HFD-induced HIF1α activation in adipose tissue. Inhibition of HIF1α in adipocytes significantly improved metabolism. [3] METHODS: In order to detect the anti-tumor activity in vivo, PX-478 (75-100 mg/kg) was intraperitoneally injected into scid mice carrying tumors OvCar-3, SHP-77, MCF-7, or PC-3 once a day for five days. RESULTS: PX-478 showed antitumor activity against established human tumor xenografts. [4] |
| 存儲條件 | store under nitrogen,keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 50 mg/mL (126.86 mM) H2O : 88.81 mM |
| 關(guān)鍵字 | Inhibitor | Autophagy | HIFs | inhibit | PX-478 | HIF-PH | HIF/HIF Prolyl-Hydroxylase | Hypoxia-inducible factors | PX478 | PX 478 |
| 相關(guān)產(chǎn)品 | Stavudine | Xylitol | Sodium 4-phenylbutyrate | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Curcumin | Hydroxycitric acid tripotassium hydrate | Oxyresveratrol | Paeonol | Naringin | Gefitinib |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | 血液病分子庫 | 抗癌臨床化合物庫 | 藥物功能重定位化合物庫 | 抑制劑庫 | 代謝化合物庫 | 抗衰老化合物庫 | 已知活性化合物庫 | 抗癌活性化合物庫 | 抗癌藥物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
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