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Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $48 | In Stock | |
5 mg | $81 | In Stock | |
10 mg | $139 | In Stock | |
25 mg | $215 | In Stock | |
50 mg | $291 | In Stock | |
100 mg | $457 | In Stock | |
1 mL x 10 mM (in DMSO) | $81 | In Stock |
Description | 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. |
In vitro | 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] |
In vivo | 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] |
Cell Research | 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]. |
Alias | PX-478 2HCl |
Molecular Weight | 394.12 |
Formula | C13H20Cl4N2O3 |
Cas No. | 685898-44-6 |
Storage | store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (126.86 mM) ![]() H2O: 88.81 mM | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
H2O/DMSO
DMSO
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