PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. PX-478 lowers HIF-1α protein levels and HIF-1 transactivation in hypoxia and in normoxia in a variety of cancer cell lines, but has a more pronounced effect on translation of proteins, such as HIF-1α in hypoxia. PX-478 also enhances the radiosensitivity of prostate carcinoma PC3 cells. PX-478 causes reduced fibrosis and fewer inflammatory infiltrates in high-fat-diet mice adipose tissues.
 |
Source | Oncotarget (2017). Figure 1. PX-478 |
| Method | Western blot | |
| Cell Lines | MiaPaCa2 cells | |
| Concentrations | 10, 20, 50, 100, and 200 μM | |
| Incubation Time | 6h | |
| Results | When MiaPaCa2 cells were exposed to the highest concentration of PX-478 and noscapine, HIF-1 expression levels equaled to 55% and 62% of the control value, respectively. |
| Molecular Weight | 394.12 |
| Formula | C13H20Cl4N2O3 |
| CAS Number | 685898-44-6 |
| Solubility (25°C) | DMSO 68 mg/mL Water 60 mg/mL |
| Storage | -20℃, dry, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related HIF Products |
|---|
| 3-Aminobenzoic acid
3-Aminobenzoic acid is a hypoxia-inducible factor-1α (HIF-1α) inhibitor. |
| Steppogenin
Steppogenin is a potent inhibitor of HIF-1α and DLL4, with IC50 values of 0.56 and 8.46 μM, respectively. |
| HIV-IN-7
Axl-IN-16 is a Axl inhibitor. |
| HIF-2α-IN-9
HIF-2α-IN-9 is an inhibitor ofHIF-2α. |
| PHD-IN-2
PHD-IN-2 is a PHD antagonist (IC50: < 5 nM). |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
