| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T55610 | ||||
| Target Name | Hypoxia-inducible factor 1 alpha (HIF-1A) | ||||
| Type of Target |
Clinical trial |
||||
| Drug Potency against Target | HIF-1alpha | Drug Info | IC50 < 2 uM/L | [3] | |
| PX-478 | Drug Info | IC50 = 2.5 uM/L | [1] | ||
| Action against Disease Model | PX-478 | Drug Info | PC3 cells were more sensitive to PX-478 as compared with DU 145 cells. Densitometric analysis showed that the IC50 for HIF-1 alpha inhibition for PC3 cells under normoxic condition was 20-25 uMol/L, whereas the IC50 for HIF-1 alpha inhibition for the DU 145 cells was 40-50 uMol/L. | [2] | |
| References | |||||
| REF 1 | Molecular mechanisms for the activity of PX-478, an antitumor inhibitor of the hypoxia-inducible factor-1alpha. Mol Cancer Ther. 2008 Jan;7(1):90-100. | ||||
| REF 2 | 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. | ||||
| REF 3 | G-rich oligonucleotides inhibit HIF-1alpha and HIF-2alpha and block tumor growth. Mol Ther. 2010 Jan;18(1):188-97. | ||||
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